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Results
- Results
Displaying 413 screens.
- Unique Compounds: 295
- Combinations: 7
- Proteins: 8
- Conditions: 5
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| Compound/Condition | Experiments | Compound/Target Mechanism | Compound Classification |
|---|---|---|---|
| 5-Fluorouracil | exp1 (2µM) exp2 (20µM) | Thymidylate synthase inhibitor, blocks DNA replication | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor |
| Actinomycin D | exp3 (1nM) exp4 (10nM) | Inhibits RNA polymerases, intercalates DNA, prevents chain elongation | Class / Subclass 1: Gene Regulation / Transcription Inhibitor |
| α-Amanitin | exp5 (500nM) | Inhibits RNA polymerase II and III, interferes with translocation | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Environmental Stresses / Toxin |
| Bortezomib | exp6 (5nM) exp7 (50nM) | Inhibits 26S proteasome, binds reversibly to chymotrypsin-like catalytic sites | Class / Subclass 1: Proteostasis / Proteasome Inhibitor |
| Brefeldin A | exp8 (20nM) | Inhibits Golgi to ER transport, forms uncompetitive complex with GBF1 and GDP-bound Arf1 | Class / Subclass 1: Organelle Function / Vesicule Trafficking Inhibitor |
| Carbonyl cyanide 3-chlorophenylhydrazone | exp10 (100nM) exp11 (1µM) | Mitochondrial proton gradient uncoupler, disrupts ATP synthesis | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor |
| Chloramphenicol | exp12 (2µM) exp13 (20µM) | Binds 23S rRNA of 50S ribosomal subunit, inhibits protein synthesis | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Organelle Function / Mitochondrial Inhibitor |
| Cycloheximide | exp14 (20nM) exp15 (200nM) | Translation elongation inhibitor, binds 60S ribosomal subunit | Class / Subclass 1: Proteostasis / Translation Inhibitor Class / Subclass 2: Environmental Stresses / Toxin |
| DABN | exp16 (2µM) exp17 (20µM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| Doxycycline | exp18 (10µM) | Inhibits bacterial 30S ribosome, also used in tet-on/tet-off gene expression control | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Organelle Function / Mitochondrial Inhibitor |
| Etoposide | exp19 (1µM) exp20 (10µM) exp198 (100nM) exp199 (300nM) | Binds DNA-TopII complex, blocks re-ligation, induces strand breaks, semi-synthetic derivative of podophyllotoxin | Class / Subclass 1: DNA Damage, Repair and Replication / Topoisomerase II Inhibitor |
| MLN-4924 | exp21 (200nM) exp22 (2µM) | Inhibits NEDD8-activating enzyme (NAE), prevents activity of cullin-RING ligase (CRL) E3 enzymes | Class / Subclass 1: Proteostasis / NEDDylation Inhibitor |
| Nocodazole | exp23 (20nM) exp24 (200nM) exp64 (200nM) exp94 (100nM) | Inhibits microtubule polymerization and mitotic spindle formation, induces spindle assembly checkpoint (SAC) | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Oligomycin A | exp25 (2µM) exp26 (20µM) | Inhibits F0 proton channel of mitochondrial ATP synthase, blocks electron flow through ETC | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor |
| Pimelic Diphenylamide 106 | exp27 (500nM) exp28 (5µM) | Inhibits HDAC3 selectively, benzamide derivative | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Rapamycin | exp307 (2µM + 3µM Cyclosporin A) exp429 (1nM) exp308 (2µM + 5µM FK-506) exp29 (1µM) exp30 (10µM) exp306 (2µM) | Allosteric mTORC1 inhibitor, forms ternary complex with FKBP12 and mTOR, attenuates protein synthesis and metabolism | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Proteostasis / mTOR inhibitor |
| Rifampicin | exp430 (30µM) exp31 (1µM) exp32 (10µM) | Inhibits bacterial RNA polymerase, induces hepatic cytochrome P450 enzymes | Class / Subclass 1: Infectious Disease / Antibiotic |
| Rotenone | exp431 (70nM) exp33 (2µM) exp34 (20µM) | Inhibits complex I, blocks electron transfer from iron-sulfur centers to ubiquinone, generates ROS, also inhibits microtubule assembly | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor Class / Subclass 2: Cell Cycle / Microtubule Poison |
| TRAIL | exp35 (5ng/mL) exp36 (50ng/mL) | TNF-related apoptosis-inducing ligand, TNF superfamily member, induces extrinsic apoptosis | Class / Subclass 1: Signal Transduction / Other Receptor Agonist |
| Wortmannin | exp37 (500nM) exp38 (5µM) | Inhibits PI3K and PI3K-related enzymes, non-specific covalent inhibitor | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Proteostasis / Autophagy Inhibitor |
| 2-Methoxyestradiol | exp310 (550nM) exp311 (0.55-0.75µM) exp312 (0.55-1µM) exp40 (200nM) | Endogenous estradiol metabolite, weak agonist for estrogen receptor, agonist of GPER1, microtubule destabilizer | Class / Subclass 1: Metabolism / Metabolite Class / Subclass 2: Signal Transduction / GPCR Agonist Class / Subclass 3: Cell Cycle / Microtubule Poison |
| BI-2536 | exp41 (1nM) exp95 (4.2nM) exp96 (20nM) | Inhibits PLK1 kinase, causes G2/M arrest | Class / Subclass 1: Cell Cycle / Mitotic Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| BI-6727 | exp42 (1nM) exp97 (12.5nM) exp98 (40nM) | Inhibits PLK1 kinase, causes G2/M arrest, improved version of BI-2536 | Class / Subclass 1: Cell Cycle / Mitotic Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Docetaxel | exp159 (0.001-0.002µM) exp45 (2nM) | Inihibts microtubule depolymerization, semi-synthetic analog of the paclitaxel | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| HMS-I1 | exp46 (1µM) exp256 (10µM) | Inhibits HDAC | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| Lapatinib | exp47 (5µM) | Inhibits EGFR and ErbB2 receptor tyrosine kinases | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Mubritinib | exp48 (200nM) exp65 (200nM) | Inhibits HER2 (Erb2) EGFR receptor tyrosine kinase | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| NFN1 | exp49 (100nM) exp99 (400nM) exp100 (1µM) | Nitrofuran derivative, candidate ALDH2 inhibitor | Class / Subclass 1: Infectious Disease / Antibiotic |
| Nicotinamide | exp50 (2000µM) exp101 (1000µM) | NAD biosynthetic precursor, activates SIRT1 | Class / Subclass 1: Metabolism / Metabolite |
| Nifuroxazide | exp51 (1µM) exp102 (5µM) | Nitrofuran antibiotic | Class / Subclass 1: Infectious Disease / Antibiotic |
| Ribavirin | exp52 (10µM) exp160 (10-15µM) | Prodrug metabolized to purine RNA nucleotide mimetic, also inhibits EIF4E | Class / Subclass 1: Infectious Disease / Antiviral Class / Subclass 2: Metabolism / Antimetabolite Class / Subclass 3: DNA Damage, Repair and Replication / Reverse Transcriptase Inhibitor |
| Suberoylanilide-Hydroxamic-Acid | exp53 (20nM) | Inhibits class I, II, IV HDACs, chelates active site zinc ion | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Paclitaxel | exp54 (2nM) exp103 (4nM) | Inhibits microtubule depolymerisation, blocks metaphase to anaphase transition | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| UM0131593 | exp58 (100nM) exp106 (200nM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| UMK57 | exp59 (1µM) exp107 (600nM) | Potentiates kinesin-13 (MCAK), destabilizes kinetochore-MT attachment, suppresses chromosome mis-segregation | Class / Subclass 1: Cell Cycle / Mitotic Inhibitor Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Vinblastine | exp208 (15nM) exp60 (2nM) exp108 (200nM) | Inhibits microtubule polymerization and mitotic spindle formation, induces spindle assembly checkpoint (SAC) | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| YM155 | exp432 (1nM) exp61 (0.2nM) | Inhibits expression of survivin, amongst other ascribed mechanisms | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Apoptosis Activator |
| BI-D1870 | exp66 (3.15µM) exp162 (2µM) | Inhibits ribosomal p90 S6 Kinase, active against RSK1/2/3/4 isoforms | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| BVD-523 | exp67 (15µM) | Inhibits ERK1/2, ATP-competitive | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Clomiphene | exp68 (4.4µM) | Nonsteroidal selective estrogen receptor modulator (SERM), mixed agonist and antagonist of ER | Class / Subclass 1: Metabolism / Hormone Antagonist Class / Subclass 2: Gene Regulation / Nuclear Receptor Ligand |
| Deguelin | exp209 (150nM) exp69 (50nM) | Derivative of rotenone, putative AKT inhibitor, complex I inhibitor | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Organelle Function / Mitochondrial Inhibitor |
| INK128 | exp70 (200nM) | Inhibits mTORC1 and mTORC2, ATP-competitive | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Proteostasis / mTOR inhibitor |
| KU-0063794 | exp71 (3.8µM) | ATP-competitive mTORC1 and mTORC2 inhibitor | Class / Subclass 1: Proteostasis / mTOR inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| LB-100 | exp72 (4.1µM) exp210 (2µM) | Inhibits protein phosphatase 2A | Class / Subclass 1: Signal Transduction / Phosphatase Inhibitor |
| LJH685 | exp73 (5µM) exp433 (50µM) | Inhibits p90 ribosomal S6 kinase (RSK) | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| MK-1775 | exp75 (320nM) | Inhibits Wee1, alleviates CDK inhibition | Class / Subclass 1: Cell Cycle / Kinase Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor Class / Subclass 3: DNA Damage, Repair and Replication / Checkpoint Signaling Inhibitor |
| Prochlorperazine | exp77 (5.2µM) | Antagonist of DRD2 receptors, used to treat nausea, schizophrenia, migraines, anxiety | Class / Subclass 1: Signal Transduction / GPCR Antagonist |
| Pterostilbene | exp78 (16µM) | Putative sirtuin activator, anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic, anti-obesity, analog of resveratrol | Class / Subclass 1: Gene Regulation / Epigenetic Activator |
| Q15 | exp79 (2.7µM) exp164 (1-2µM) | Putative condensin inhibitor | Class / Subclass 1: Cell Cycle / Chromosome Dynamics Inhibitor |
| RO-3306 | exp80 (4.7µM) exp165 (3-4µM) | Inhibits CDK1, ATP-competitive, causes G2/M arrest | Class / Subclass 1: Cell Cycle / Kinase Inhibitor |
| Selumetinib | exp81 (20µM) | Inhibits MEK1 and MEK2 | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Torin1 | exp82 (80nM) | Inhibits mTORC1 and mTORC2, ATP competitive | Class / Subclass 1: Proteostasis / mTOR inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Trametinib | exp83 (10µM) | Inhibits MEK1 and MEK2, reversible allosteric mechanism, used in combination with BRAF V600E inhibitors | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| UM0125461 | exp84 (740nM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| UM0129480 | exp85 (7µM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| Vemurafenib | exp434 (6.6µM) exp89 (6.6µM) | Inhibits BRAF-V300E, paradoxical RAF activation by stabilization of CRAF/BRAF heterodimer | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| WYE-354 | exp90 (6µM) | Inhibits mTORC1 and mTORC2, ATP-competitive inhibitor | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Proteostasis / mTOR inhibitor |
| (R)-DABN | exp93 (10µM + 10µM (S)-DABN) exp111 (8µM) | Unknown, (R) atropisomer of 1,1'-Binaphthyl-2,2'-diamine | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| (S)-DABN | exp93 (10µM + 10µM (R)-DABN) exp112 (8µM) | Unknown, (S) atropisomer of 1,1'-Binaphthyl-2,2'-diamine | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| 1-Methylnicotinamide chloride | exp113 (1000µM) | Nicotinamde metabolite, generated by nicotinamide N-methyltransferase (NNMT) | Class / Subclass 1: Metabolism / Metabolite |
| A-196 | exp114 (10µM) | Inhibits SUV420H1 and SUV420H2 inhibitor, blocks di/trimethylation of H4K20me | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| A-366 | exp115 (10µM) | Inhibits G9a/EHMT1, blocks methylation of H3K9 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| AICAR | exp116 (240µM) exp211 (240µM) | Metabolic intermediate in purine biosynthesis, activates AMPK, has other putative targets | Class / Subclass 1: Metabolism / Metabolite Class / Subclass 2: Signal Transduction / Kinase Activator |
| BH1 | exp169 (1µM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| DMSO | exp120 (1%) | N/A | Class / Subclass 1: Chemogenomic Negative Control / Solvent |
| Golgicide A | exp121 (2µM) exp122 (4µM) | Inhibits cis-Golgi ArfGEF, blocks secretion at ER-Golgi | Class / Subclass 1: Organelle Function / Vesicule Trafficking Inhibitor |
| GSK-LSD1 | exp123 (10µM) | Inhibits LSD1 histone demethylase (H3K4me/me2, H3K9me) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| GSK343 | exp124 (3µM) | Inhibits EZH1 catalytic subunit of PRC2 histone methyltransferase (H3K27me3) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| GSK461364A | exp125 (5nM) exp126 (100nM) | Inhibits PLK1 | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Cell Cycle / Mitotic Inhibitor |
| GSK591 | exp128 (2.6µM) | Inhibits protein arginine methyltransferase PRMT5, inactive control is SGC2096 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Isonicotinamide | exp129 (500µM) | nicotinamide antagonist, putative SIRT1 activator | Class / Subclass 1: Metabolism / Metabolite |
| JQ1 | exp435 (800nM) exp130 (10nM) | Inhibits BET bromodomain proteins BRD2, BRD3, BRD4, BRDT | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| L-741,742 | exp131 (5µM) | DRD4 receptor antagonist | Class / Subclass 1: Signal Transduction / GPCR antagonist |
| Metformin | exp132 (40µM) exp170 (100-150µM) | Inhibits mitochondrial respiratory chain complex I, indirectly activates AMPK | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor Class / Subclass 2: Signal Transduction / Kinase Activator |
| MKC9989 | exp133 (10µM) | Inhibits IRE1, prevents ER unfolded protein response | Class / Subclass 1: Proteostasis / Unfolded Protein Response Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| MS023 | exp134 (2µM) exp135 (7µM) | Inhibits protein arginine N-methyltransferase PRMT1 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| MS094 | exp136 (2µM) | Inactive control for MS023 PRMT1 inhibitor | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Nicotinamide Riboside | exp139 (100µM) | NAD precursor, activates SIRT1 | Class / Subclass 1: Metabolism / Metabolite |
| Nicotinate | exp140 (1000µM) | NAD precursor (a.k.a. niacin, vitamin B3) | Class / Subclass 1: Metabolism / Metabolite |
| Nifurtimox | exp141 (1µM) | Nitrofuran derivative, forms nitro-anion radical metabolite, induces ROS | Class / Subclass 1: Infectious Disease / Antitrypanosomal |
| OICR-9429 | exp142 (10µM) | Inhibits interaction between WDR5 and MLL1 (KMT2A) in MLL H3K4 trimethylase complex | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Phenformin | exp143 (20µM) exp212 (20µM) | Inhibits mitochondrial respiratory chain complex I, indirectly activates AMPK | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor Class / Subclass 2: Metabolism / Metabolic Enzyme Activator |
| PFI-3 | exp144 (10µM) | Inhibits SMARCA2/4 and PB1 bromodomain proteins, components of SNF/SWI chromatin remodelling complex | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| PNU96415E | exp145 (10µM) | Antagonist of DRD4 and 5-HT2A receptors | Class / Subclass 1: Signal Transduction / GPCR Antagonist |
| Quinacrine | exp146 (2.5µM) | Intercalates into DNA and RNA, interferes with transcription and translation | Class / Subclass 1: Infectious Disease / Antimalarial Class / Subclass 2: DNA Damage, Repair and Replication / Intercalating Agent |
| Resveratrol | exp147 (16µM) | Putative sirtuin activator, many other ascribed activities, analog of pterostilbene | Class / Subclass 1: Gene Regulation / Epigenetic Activator |
| SB202190 | exp148 (10µM) | Inhibits p38‘± (MAPK14)and p38‘_ (MAPK11) kinase, ATP competitive | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| SB203580 | exp149 (25µM) | p38 MAP kinase inhibitor | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Proteostasis / Autophagy Inhibitor |
| SGC0649 | exp150 (7µM) | Inactive control for SGC0649 (DOT1L methyltransferase inhibitor) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| SGC0946 | exp151 (7µM) | DOT1L methyltransferase inhibitor | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| SGC2043 | exp152 (10µM) | Inactive control for A-196 (SUV420H1/H2 inhibitor) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| SGC2096 | exp153 (2.6µM) | Inactive control for GSK591 (PRMT5 inhibitor) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| UNC1999 | exp155 (2µM) | Inhibits EZH2 catalytic subunit of PRC2 histone methyltransferase (H3K27me3) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| UNC2400 | exp156 (2µM) | Inactive control for UNC1999 (EZH2 inhibitor) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| 2-Deoxy-D-glucose | exp214 (800µM) | Inhibits phosphoglucoisomerase, competitive, blocks glycolysis | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| 3-Bromopyruvate | exp175 (7µM) | Inhibits hexokinase II, pyruvate analog, enzyme alkylator, blocks glycolysis | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| Apcin | exp177 (25µM + 2µM proTAME) exp176 (50-100µM) | Inhibits substrate interactions with APC/C-Cdc20 | Class / Subclass 1: Proteostasis / E3 ubiquitin ligase inhibitor Class / Subclass 2: Cell Cycle / Mitotic Inhibitor |
| Colchicine | exp215 (9nM) | Inhibits microtubule polymerization | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Combretastatin A4 | exp179 (0.002-0.003µM) | Inhibits microtubule polymerization | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Dynasore | exp436 (7µM) exp180 (10µM) | Putative dynamin GTPase inhibitor, blocks endocytosis | Class / Subclass 1: Organelle Function / Vesicule Trafficking Inhibitor |
| Erlotinib | exp216 (10µM) | Inhibits EGFR, also cyclin G-associated kinase (GAK) | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| IU1-47 | exp182 (25µM) | Inhibits USP14, enhances protein degradation by 26S proteasome | Class / Subclass 1: Proteostasis / Deubiquitinase (DUB) Inhibitor |
| IU1-C | exp183 (25µM) | Inactive analog of IU1-47 | Class / Subclass 1: Proteostasis / Ubiquitin-Proteasome Inhibitor |
| Ixabepilone | exp184 (0.004-0.005µM) | Inhibits microtubule depolymerization, semi-synthetic analog of epothilone | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| L-BMAA | exp185 (500-750µM) | ‘_-Methylamino-l-alanine, cyanobacterial neurotoxin, possible causative agent of ALS | Class / Subclass 1: Environmental Stresses / Toxin |
| Mdivi-1 | exp217 (15µM) | Inhibits GTPase dynamin-related protein 1 (Drp1), impairs mitochondrial fission, also inhibits respiratory complex I | Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor |
| proTAME | exp177 (2µM + 25µM Apcin) exp187 (5µM) | Inhibits APC/C interaction with Cdc20/Cdh1 substrate recognition cofactors | Class / Subclass 1: Proteostasis / E3 ubiquitin ligase inhibitor Class / Subclass 2: Cell Cycle / Mitotic Inhibitor |
| Temozolomide | exp189 (200µM) | Alkylates purine bases, prodrug hydrolyzes to 3-methyl-(triazen-1-yl)imidazole-4-carboxamide (MTIC) | Class / Subclass 1: DNA Damage, Repair and Replication / Base Alkylation |
| Vincristine | exp190 (0.5nM) | Inhibits microtubule polymerization and mitotic spindle formation, induces spindle assembly checkpoint (SAC) | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| A-395 | exp218 (10µM) | Inhibits EED subunit of PRC2 complex, blocks H3K27me3 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| A-395N | exp219 (10µM) | Inactive analog of A-395 EED inhibitor | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| BAY-598 | exp220 (4µM) | Inhibits SMYD2 lysine methyltransferase that acts on H3K4me, H3K36me, p53 and other substrates | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Betulinic acid | exp222 (10-15µM) | Pentacyclic triterpenoid, claimed antiretroviral, antimalarial, anti-inflammatory, topoisomerase I/II inhibitor | Class / Subclass 1: Infectious Disease / Antiviral Class / Subclass 2: DNA Damage, Repair and Replication / DNA Damaging Agent Class / Subclass 3: Uncharacterized Mechanism / Natural Product |
| Cabazitaxel | exp223 (1nM) | Microtubule stabilizer, semi-synthetic taxane | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| CB-839 | exp224 (10µM) | Inhibits glutaminase (GLS1), reversible | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| Celastrol | exp225 (120nM) | Putative antioxidant, anti-inflammatory, antiobesity anticancer, proteasome inhibitor | Class / Subclass 1: Uncharacterized Mechanism / Natural Product Class / Subclass 2: Proteostasis / Ubiquitin-Proteasome Inhibitor |
| Cerivastatin | exp226 (150nM) | Inhibits HMG-CoA reductase, decreases cholesterol biogenesis, upregulates LDL receptors | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| Cryptotanshinone | exp227 (12µM) | Putative acetylcholinesterase and STAT3 inhibitor | Class / Subclass 1: Uncharacterized Mechanism / Natural Product |
| Demecolcine | exp228 (30nM) | Inhibits microtubule polymerization, a.k.a. colcemid | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Dimethyloxaloylglycine | exp314 (11µM) exp229 (100µM) exp319 (11µM + 5µM ABT-702) | Prolylhydroxylase inhibitor, induces HIF-1α accumulation | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor Class / Subclass 2: Signal Transduction / Other inhibitor |
| Epigallocatechin gallate | exp230 (20µM) | Polyphenol antioxidant from green tea, numerous claimed activities | Class / Subclass 1: Metabolism / Nutraceutical Class / Subclass 2: Environmental Stresses / Food Additive |
| Epothilone B | exp231 (1.5nM) | Inhibits microtubule depolymerization, parent compound of ixabepilone | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| Epothilone D | exp232 (4-6nM) | Microtubule stabilizer | Class / Subclass 1: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 2: Cell Cycle / Microtubule Poison |
| EPZ-5676 | exp233 (30µM) | Inhibits DOT1L lysine methyltransferase (H3K79me2) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Ethanol | exp234 (1%) exp437 (0.3%) | Pleiotropic effects on membranes, ion channels, enzymes, receptors | Class / Subclass 1: Environmental Stresses / Solvent |
| Geldanamycin | exp235 (10nM) exp316 (0.015-0.025µM) exp317 (0.015-0.05µM) | HSP90 inhibitor | Class / Subclass 1: Proteostasis / Chaperone Inhibitor |
| GSK2606414 | exp236 (1µM) | Inhibits PERK, also KIT receptor | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| N,N-Diethyl-3-methylbenzamide | exp237 (100µM) exp438 (500µM) | Insect repellent | Class / Subclass 1: Environmental Stresses / Environmental Contaminant |
| Parthenolide | exp238 (2.5µM) | Sesquiterpene lactone with attributed activities in microtubule function, NF-κB activation, HDAC1 inhibition, MDM2 ubiquitination. Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Uncharacterized Mechanism / Natural Product Class / Subclass 3: Signal Transduction / Apoptosis Inducer |
| PFI-2 | exp239 (4µM) | Inhibits SETD7 lysine methyltransferase (H3K4me) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Pyridostatin | exp240 (4µM) | Binds and stabilizes telomeric and interstitial G-quadruplexes | Class / Subclass 1: DNA Damage, Repair and Replication / G-Quadruplex Stabilizer |
| QNZ | exp439 (10nM) exp241 (10nM) | Inhibits NF-κB activation, TNF-α production | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Apoptosis Inhibitor |
| Radicicol | exp242 (160nM) | Inhibits HSP90 | Class / Subclass 1: Proteostasis / Chaperone Inhibitor Class / Subclass 2: Infectious Disease / Antifungal |
| S-Trityl-L-cysteine | exp243 (500nM) | Inhibits Eg5 kinesin, blocks centrosome separation and bipolar spindle formation, arrests cells with monoastral spindles | Class / Subclass 1: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 2: Cell Cycle / Microtubule Poison |
| SB743921 | exp244 (1nM) | Inhibits Eg5 kinesin, derivative of S-trityl-L-cysteine | Class / Subclass 1: Cell Cycle / Mitotic Inhibitor |
| UM0011500 | exp245 (5µM) exp246 (10µM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| UM0130462 | exp247 (0.025-0.035µM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| UM0131023 | exp248 (50nM) | Unknown | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| Vinorelbine | exp249 (1nM) | Inhibits microtubule polymerization and mitotic spindle formation, induces spindle assembly checkpoint (SAC) | Class / Subclass 1: Cell Cycle / Microtubule Poison Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor |
| 6-Thioguanine | exp259 (2µM) | Nucleoside analog, incorporated into telomeric DNA by telomerase, impairs proliferation of telomerase-positive cells | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: DNA Damage, Repair and Replication / Helix-Distorting Adduct |
| ABT-702 | exp320 (5µM + 18µM CoCl2) exp318 (5µM) exp321 (5µM + 11µM Deferoxamine) exp319 (5µM + 11µM Dimethyloxaloylglycine) exp260 (100nM) exp261 (5µM) | Inhibits adenosine kinase (ADK) | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| ALDA-1 | exp262 (10µM) | Activates mitochondrial aldehyde dehydrogenase (ALDH2), may attenuate ethanol addiction | Class / Subclass 1: Metabolism / Metabolic Enzyme Activator |
| Aphidicolin | exp440 (400nM) exp263 (40nM) | Inhibits DNA polymerases Polα, Polδ, Polϵ and Polζ | Class / Subclass 1: DNA Damage, Repair and Replication / Replication Inhibitor Class / Subclass 2: Cell Cycle / Replication Inhibitor Class / Subclass 3: Infectious Disease / Antiviral |
| Arsenate | exp264 (40µM) | Heavy metal toxin, environmental contaminant | Class / Subclass 1: Environmental Stresses / Heavy Metal |
| Bisphenol A | exp269 (100µM) | Widely-used in plastics and epoxy resins, endocrine disrupter | Class / Subclass 1: Environmental Stresses / Industrial Chemical |
| Camptothecin | exp270 (1nM) | Inhibits topoisomerase I, stabilizes TopoI-DNA complex, causes DNA strand breaks | Class / Subclass 1: DNA Damage, Repair and Replication / Clastogen |
| CCT251545 | exp271 (200nM) exp326 (20µM) | Inhibits CDK8 and CDK19 mediator-associated kinases | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| CHIR-124 | exp272 (40nM) | Inhibits CHK1, blocks checkpoint arrest, potentiates DNA damaging agents | Class / Subclass 1: DNA Damage, Repair and Replication / Checkpoint Signaling Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Cisplatin | exp273 (350nM) | Intrastrand cross-linker | Class / Subclass 1: DNA Damage, Repair and Replication / Inter/Intra-strand Crosslinker |
| Citral | exp274 (50µM) exp275 (75µM) | putative ALDH inhibitor, essential oil | Class / Subclass 1: Uncharacterized Mechanism / Natural Product Class / Subclass 2: Metabolism / Metabolic Enzyme Inhibitor |
| Curcumin | exp277 (6.5µM) | Component of tumeric spice, many claimed activities but viewed as pan-assay interference compound | Class / Subclass 1: Uncharacterized Mechanism / Natural Product Class / Subclass 2: Metabolism / Nutraceutical |
| CVT-10216 | exp278 (100nM) | Inhibits mitochondrial aldehyde dehydrogenase (ALDH2), main enzyme for oxidative alcohol metabolism | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| D-Fructose | exp279 (10000µM) | Monosaccharide | Class / Subclass 1: Metabolism / Nutrient |
| Daidzin | exp280 (10µM) | Isoflavone from soy bean, putative ALDH inhibitor | Class / Subclass 1: Uncharacterized Mechanism / Natural Product Class / Subclass 2: Metabolism / Metabolic Enzyme Inhibitor |
| Disulfiram | exp281 (4.3µM) | ALDH1 inhibitor, putative 26S proteasome inhibitor | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor Class / Subclass 2: Proteostasis / Ubiquitin-Proteasome Inhibitor |
| Fluvastatin | exp282 (2.2µM) | Inhibits HMG-CoA reductase, decreases cholesterol biogenesis, upregulates LDL-receptors | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| Glyphosate | exp283 (1000µM) | Inhibits 5-enolpyruvylshikimate-3-phosphate synthase, a.k.a Roundup | Class / Subclass 1: Environmental Stresses / Herbicide |
| GW501516 | exp285 (25µM) | PPARδ receptor agonist, increases metabolism, banned performance enhancer | Class / Subclass 1: Gene Regulation / Nuclear Receptor Ligand Class / Subclass 2: Metabolism / Hormone Agonist |
| HMS-I2 | exp286 (1µM) exp287 (5µM) exp288 (10µM) | putative HDAC inhibitor from cell-based screen | Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit |
| Hydroxyurea | exp329 (100µM) exp289 (15µM) | Inhibits ribonucleotide reductase, scavenges tyrosyl radicals | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor |
| LLY-283 | exp290 (2.6µM) | Inhibits protein arginine methyltransferase PRMT5, inactive control is LLY-284 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| LLY-284 | exp291 (2.6µM) | Inactive control for LLY-283 PRMT5 inhibitor | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Menadione | exp292 (5µM) | Synthetic analog of vitamin K, quinone redox cycle generates ROS | Class / Subclass 1: Metabolism / Nutrient Class / Subclass 2: Environmental Stresses / Food Additive |
| Myriocin | exp293 (25µM) | Inhibits serine palmitoyltransferase (SPT1), sphingolipid biosynthesis | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Metabolism / Metabolic Enzyme Inhibitor |
| Nutlin-3A | exp294 (1.6µM) | Inhibits p53-MDM2 interaction | Class / Subclass 1: Proteostasis / E3 ubiquitin ligase inhibitor Class / Subclass 2: Signal Transduction / Apoptosis Activator |
| Pyronaridine | exp295 (1µM) | Prevents sequestration of heme into hemozoin, forms toxic complex with heme, enhances hematin-induced red blood cell lysis, also intercalates into DNA | Class / Subclass 1: Infectious Disease / Antimalarial Class / Subclass 2: DNA Damage, Repair and Replication / Intercalating Agent |
| Sucrose | exp298 (20000µM) | Disaccharide composed of glucose and fructose | Class / Subclass 1: Metabolism / Nutrient |
| Talazoparib | exp299 (6nM) | Inhibits PARP1 and PARP2, blocks ssDNA break repair, selectively toxic to BRCA1/2 negative cancers | Class / Subclass 1: DNA Damage, Repair and Replication / PARP Inhibitor |
| VE-822 | exp300 (40nM) | Inhibits ATR | Class / Subclass 1: DNA Damage, Repair and Replication / Checkpoint Signaling Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| VER-155008 | exp301 (3.9µM) | Inhibits HSP70 | Class / Subclass 1: Proteostasis / Chaperone Inhibitor |
| 5-Azacytidine | exp330 (2µM) | Analog of cytidine ribonucleoside, DNA methyltransferase inhibitor | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: Gene Regulation / Epigenetic Inhibitor Class / Subclass 3: DNA Damage, Repair and Replication / Replication Inhibitor |
| A-769662 | exp331 (20µM) | Activates AMP-activated protein kinase (AMPK), allosteric | Class / Subclass 1: Signal Transduction / Kinase Activator |
| Adefovir | exp332 (20µM) | Nucleoside reverse transcriptase inhibitor (NRTI), active against HBV and HSV | Class / Subclass 1: Infectious Disease / Antiviral Class / Subclass 2: DNA Damage, Repair and Replication / Reverse Transcriptase Inhibitor Class / Subclass 3: Metabolism / Antimetabolite |
| Tretinoin | exp333 (8µM) exp334 (40µM) | Ligand for retinoic acid receptor (RAR) and retinoid X receptor (RXR), metabolite of vitamin A1 | Class / Subclass 1: Gene Regulation / Nuclear Receptor Ligand Class / Subclass 2: Metabolism / Metabolite |
| Aminopterin | exp335 (5nM) | Inhibits dihydrofolate reductase (DHFR) | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor |
| Asunaprevir | exp336 (3µM) | Block the enzymatic activity of the HCV NS3 protease | Class / Subclass 1: Infectious Disease / Antiviral Class / Subclass 2: Proteostasis / Protease Inhibitor |
| BN82002 | exp340 (4µM) | Inhibits CDC25 phosphatases, active against CDC25A/B/C isoforms | Class / Subclass 1: Cell Cycle / Phosphatase inhibitor Class / Subclass 2: Signal Transduction / Phosphatase Inhibitor |
| BIC1 | exp341 (20µM) | Inhibits BRD2, blocks recognition of acetylated H4K12 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| A23187 | exp342 (400nM) | Calcium ionophore | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Organelle Function / Membrane Ionophore |
| Centrinone | exp343 (500nM) | Inhibits PLK4, blocks centriole duplication, causes p53-dependent G1 arrest | Class / Subclass 1: Cell Cycle / Mitotic Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Chlorpromazine | exp344 (10µM) | Antipsychotic, pleiotropic antagonist for dopamine, seratonin, histamine, adrenergic, muscarinic receptors, potassium and sodium channels, also disrupts clathrin-mediated endocytosis | Class / Subclass 1: Signal Transduction / GPCR Antagonist Class / Subclass 2: Signal Transduction / Ion Channel Inhibitor Class / Subclass 3: Organelle Function / Vesicule Trafficking Inhibitor |
| Cidofovir | exp345 (10µM) | Acyclic nucleoside phosphonate, inhibits DNA polymerase | Class / Subclass 1: Infectious Disease / Antiviral Class / Subclass 2: Metabolism / Antimetabolite Class / Subclass 3: DNA Damage, Repair and Replication / Replication Inhibitor |
| CoCl2 | exp320 (18µM + 5µM ABT-702) exp346 (18µM) | Hypoxia mimetic, inhibits VHL-HIF-1α interaction, induces HIF-1α accumulation | Class / Subclass 1: Environmental Stresses / Heavy Metal |
| Cyclosporin A | exp307 (3µM + 2µM Rapamycin) exp347 (800nM) exp348 (3µM) | Inhibits calcineurin, forms ternary complex with immunophilin (FBKP) and calcineurin | Class / Subclass 1: Signal Transduction / Phosphatase Inhibitor Class / Subclass 2: Proteostasis / mTOR inhibitor |
| Cytochalasin B | exp349 (5µM) | Binds fast-growing (barbed) end of F-actin filament, inhibits actin polymerization | Class / Subclass 1: Cell Cycle / Cytokinesis Inhibitor Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 3: Environmental Stresses / Toxin |
| Deferoxamine | exp321 (11µM + 5µM ABT-702) exp350 (11µM) | Iron chelator, hypoxia mimetic, induces HIF-1‘± accumulation | Class / Subclass 1: Environmental Stresses / Metal Chelator |
| Dexamethasone | exp351 (6nM) exp352 (0.006-0.015µM) | Glucocorticoid receptor agonist, anti-inflammatory | Class / Subclass 1: Metabolism / Hormone Agonist Class / Subclass 2: Signal Transduction / GPCR Agonist |
| Diepoxybutane | exp354 (3µM) | DNA crosslinker, carcinogen | Class / Subclass 1: DNA Damage, Repair and Replication / Inter/Intra-strand Crosslinker |
| Dinaciclib | exp355 (7nM) | Inhibits CDK2, CDK5, CDK1, CDK9 | Class / Subclass 1: Cell Cycle / Cell Cycle Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor Class / Subclass 3: Gene Regulation / Transcription Inhibitor |
| Docosahexaenoic acid | exp356 (50µM) | Essential omega-3 fatty acid | Class / Subclass 1: Metabolism / Metabolite |
| Dorsomorphin | exp357 (5µM) | Putative inhibitor of AMPK and BMP signalling | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| FK-506 | exp308 (5µM + 2µM Rapamycin) exp358 (5µM) exp359 (30µM) | Inhibits calcineurin | Class / Subclass 1: Signal Transduction / Phosphatase Inhibitor Class / Subclass 2: Proteostasis / mTOR inhibitor |
| Genistein | exp360 (15µM) | Inhibits tyrosine kinases, phytoestrogen, toposiomerase II, pleiotropic effects | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Metabolism / Hormone Agonist Class / Subclass 3: Gene Regulation / Nuclear Receptor Ligand |
| GSK-J4 | exp362 (1µM) exp363 (1-1.25µM) exp441 (1.5µM) | JMJD3/KDM6B, UTX/KDM6A histone demethylase inhibitor (H3K27me2/me3) | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| I-BRD9 | exp365 (4µM) | Inhibits BRD9 subunit of SWI/SNF complex | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Ibrutinib | exp372 (1µM) exp442 (10µM) | Inhibits BTK | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Latrunculin B | exp374 (10µM) | Binds actin monomers, inhibits actin polymerization | Class / Subclass 1: Cell Cycle / Cytokinesis Inhibitor Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 3: Environmental Stresses / Toxin |
| Lenalidomide | exp375 (20µM) | IMiD that targets IKZF1/3 for ubiquitination by CUL4-cereblon complex | Class / Subclass 1: Proteostasis / Bivalent Ligand |
| Losmapimod | exp376 (1µM) | Inhibits p38‘±/‘_ MAP kinases | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| MSC2530818 | exp379 (10µM) | Inhibits CDK8 | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| NMS-873 | exp380 (70nM) | Inhibits p97 AAA-ATPase | Class / Subclass 1: Proteostasis / Ubiquitin-Proteasome Inhibitor |
| Palbociclib | exp382 (1µM) | Inhibits CDK4 and CDK6, causes G1 arrest | Class / Subclass 1: Cell Cycle / Cyclin Dependent Kinase Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| PF-06409577 | exp389 (20µM) | Activates AMPK, lowers cholesterol levels in NAFLD/NASH preclinical models | Class / Subclass 1: Signal Transduction / Kinase Activator |
| Pifithrin-α | exp390 (20µM) | Claimed to inhibit p53 but has p53-independent effects, cyclic form may increase stem cell reprogramming | Class / Subclass 1: Signal Transduction / Apoptosis Inhibitor |
| Pomalidomide | exp391 (20µM) | IMiD that targets neo-substrates IKZF1/3 for ubiquitination by CUL4A-DDB1-cereblon complex | Class / Subclass 1: Proteostasis / Ubiquitin-Proteasome Activator |
| PT 1 | exp392 (25µM) | Activates AMPK, selectivefor ‘_1-complexes, may antagonize autoinhibition | Class / Subclass 1: Signal Transduction / Kinase Activator |
| Resminostat | exp393 (500nM) | Inhibits HDAC 1, HDAC3, HDAC6 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Salubrinal | exp399 (20µM) | Inhibits eIF2‘± phosphatase, indirectly inhibits eIF2‘± | Class / Subclass 1: Proteostasis / Translation Inhibitor |
| Senexin A | exp400 (25µM) | Inhibits CDK8, suppresses induction of gene expression | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Gene Regulation / Transcription Inhibitor |
| SNS-032 | exp401 (25µM) exp443 (15µM) | Inhibits CDK2, CDK7, CDK9 | Class / Subclass 1: Cell Cycle / Cyclin Dependent Kinase Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Tenofovir | exp405 (10µM) | Nucleoside reverse transcriptase inhibitor, chain terminator | Class / Subclass 1: Infectious Disease / Antiviral |
| Thalidomide | exp406 (20µM) | IMiD that targets neo-substrates IKZF1/3 for ubiquitination by CUL4A-DDB1-cereblon complex | Class / Subclass 1: Proteostasis / Bivalent Ligand |
| Thapsigargin | exp407 (5nM) | Inhibits sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), non-competitive inhibitor, raises intracellular calcium concentration | Class / Subclass 1: Organelle Function / Membrane Transport Inhibitor Class / Subclass 2: Signal Transduction / Ion Channel Inhibitor |
| THZ531 | exp409 (110nM) exp410 (0.11-0.125µM) exp412 (0.11-0.35µM) exp413 (0.11-0.175µM) exp444 (225nM) | Inhibits CDK12 and CDK13, forms covalent adduct, more selective analog of THZ1, blocks phosphorylation of the C-terminal domain of RNA polymerase II | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Tozasertib | exp414 (100nM) | Inhibits Aurora A,B,C kinases, blocks cytokinesis, also inhibits RIPK1 and blocks necroptosis | Class / Subclass 1: Cell Cycle / Cytokinesis Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Trichostatin A | exp415 (60nM) | Inhibits class I and II HDAC enzymes | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor Class / Subclass 2: Infectious Disease / Antifungal |
| Tubacin | exp416 (1.6µM) | Inhibits HDAC6 selectively | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Tubastatin A | exp417 (2.5µM) | Inhibits HDAC6 selectively | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| Tunicamycin | exp418 (40nM) exp419 (0.04-0.075µM) exp420 (0.04-0.125µM) | Inhibits GlcNAc phosphotransferase (GPT), blocks N-linked glycoslylation, induces protein unfolding in ER, nucleoside antibiotic | Class / Subclass 1: Proteostasis / Unfolded Protein Response Activator Class / Subclass 2: Infectious Disease / Antibiotic |
| VHL Ligand 1 | exp421 (20µM) | Binds VHL, targeting moiety for PROTACs | Class / Subclass 1: Proteostasis / Bivalent Ligand |
| Wiskostatin | exp422 (3µM) | Inhibits N-WASP, blocks actin polymerization | Class / Subclass 1: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 2: Cell Cycle / Actin Inhibitor |
| Zebularine | exp423 (20µM) | Inhibits cytidine deaminase, transition state analog, also inhibits DNMT1 via reversible covalent complex | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| β-Estradiol | exp425 (550nM) | Agonist for estrogen receptor (ER), inactive control for 2-Methoxyestradiol | Class / Subclass 1: Gene Regulation / Transcription Activator Class / Subclass 2: Metabolism / Hormone Agonist |
| ∆9-Tetrahydrocannabinol | exp445 (30µM) | Agonist of CB1 and CB2 cannabinoid receptors | Class / Subclass 1: Environmental Stresses / Controlled Substance Class / Subclass 2: Signal Transduction / GPCR Agonist |
| 4-Nitroquinoline N-oxide | exp446 (500nM) | UV mimetic, metabolized to electrohpile that forms stable quinolone monoadducts | Class / Subclass 1: DNA Damage, Repair and Replication / Helix-Distorting Adduct |
| Amiloride | exp447 (100µM) | Inhibits epithelial sodium channel (ENaC) and other Na+/H+ channels, also inhibits urokinase-type plasminogen activator (uPA) | Class / Subclass 1: Signal Transduction / Ion Channel Inhibitor |
| Ammonium tetrathiomolybdate | exp448 (10µM) | Inhibits cuproenzymes superoxide dismutase 1 (SOD1) and cytochrome c oxidase (COX) | Class / Subclass 1: Environmental Stresses / Metal Chelator Class / Subclass 2: Metabolism / Metabolic Enzyme Inhibitor |
| Arsenic trioxide | exp449 (60µM) | Induces degradation of aberrant PML-RAR‘± fusion protein in acute promyelocytic leukemia | Class / Subclass 1: Environmental Stresses / Heavy Metal Class / Subclass 2: Signal Transduction / Apoptosis Inducer |
| Artemisinin | exp450 (50µM) | Sesquiterpene endoperoxide activated by heme, kills malaria parasite through oxidative damage | Class / Subclass 1: Infectious Disease / Antimalarial |
| Atovaquone | exp451 (15µM) | Ubiquinone analog, inhibits mitochondrial complex III, induces DNA strand breaks | Class / Subclass 1: Infectious Disease / Antimalarial Class / Subclass 2: Organelle Function / Mitochondrial Inhibitor Class / Subclass 3: DNA Damage, Repair and Replication / DNA Damaging Agent |
| Azithromycin | exp452 (100µM) | Binds 50S subunit of bacterial ribosome, inhibits translation | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Proteostasis / Translation Inhibitor |
| B02 | exp453 (10µM) | Inhibits RAD51 recombinase, blocks homologous recombination | Class / Subclass 1: DNA Damage, Repair and Replication / Repair Protein Inhibitor |
| Bafilomycin A1 | exp454 (9nM) | Inhibits vacuolar-type H+ ATPase, blocks acidification of lysosome | Class / Subclass 1: Signal Transduction / Ion Channel Inhibitor Class / Subclass 2: Organelle Function / Membrane Transport Inhibitor Class / Subclass 3: Proteostasis / Autophagy Inhibitor |
| Benzoate | exp455 (10000µM) exp456 (20000µM) | Food additive (E211), bacteriostatic and fungistatic | Class / Subclass 1: Environmental Stresses / Food Preservative |
| Bisphenol F | exp457 (50µM) | BPA analog and substitute, endocrine disrupter | Class / Subclass 1: Environmental Stresses / Industrial Chemical |
| Bisphenol S | exp458 (100µM) | BPA analog and substitute in BPA-free plastics, endocrine disrupter | Class / Subclass 1: Environmental Stresses / Industrial Chemical |
| Bleomycin | exp459 (5µM) | Induces DNA strand breaks, possibly by iron chelation and ROS generation, or generation of alkali-labile lesions | Class / Subclass 1: DNA Damage, Repair and Replication / Clastogen |
| BML-284 | exp460 (90nM) | Wnt agonist, GSK3-‘_ dependent, activates ‘_-catenin/TCF-dependent transcription | Class / Subclass 1: Signal Transduction / GPCR Agonist Class / Subclass 2: Gene Regulation / Transcription Activator |
| BS-181 | exp461 (20µM) | Inhibits CDK7, causes G1 arrest and apoptosis | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Cadmium | exp462 (60µM) | Widely used metal in manufacturing and pigments, known carcinogen | Class / Subclass 1: Environmental Stresses / Heavy Metal |
| Caffeine | exp463 (2600µM) | CNS stimulant, antagonist of adenosine receptors, inhibits phosphodiesterases, modulates intracellular calcium | Class / Subclass 1: Signal Transduction / GPCR Antagonist Class / Subclass 2: Environmental Stresses / Food Additive |
| Calcipotriol | exp464 (5µM) | Synthetic vitamin D3 analog, binds vitamin D nuclear hormone receptor | Class / Subclass 1: Metabolism / Vitamin Class / Subclass 2: Signal Transduction / Nuclear Receptor Ligand |
| Cannabidiol | exp465 (13µM) exp466 (20µM) | Negative allosteric modulator of cannabinoid CB1 receptor | Class / Subclass 1: Environmental Stresses / Psychoactive Drug Class / Subclass 2: Signal Transduction / GPCR Antagonist |
| CAY10603 | exp467 (550nM) | Inhibits HDAC6, selective over other HDACs | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| CB-5083 | exp468 (400nM) | Inhibits p97 AAA-ATPase | Class / Subclass 1: Proteostasis / Unfoldase Inhibitor |
| CFI-400945 | exp469 (25µM) | Inhibits PLK4, blocks centriole duplication, induces mitotic defects and cell death | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Cell Cycle / Mitotic Inhibitor |
| Chloroquine | exp470 (32µM) | Lysosomotropic agent, prevents sequestration of heme into hemozoin, forms toxic complex with heme, enhances hematin-induced red blood cell lysis, also intercalates into DNA | Class / Subclass 1: Infectious Disease / Antimalarial Class / Subclass 2: DNA Damage, Repair and Replication / Intercalating Agent Class / Subclass 3: Proteostasis / Autophagy Inhibitor |
| Cholesterol | exp471 (3-100nM) | Major membrane lipid, precursor for the biosynthesis of steroid hormones, bile acids, and vitamin D | Class / Subclass 1: Metabolism / Metabolite |
| CI-1040 | exp472 (9.5µM) | Inhibits MEK1, blocks ERK1/2 activation | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Cincreasin | exp473 (100µM) | Inhibits budding yeast Mps1 but not human MPS1 (TTK), overrides spindle checkpoint | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor Class / Subclass 3: Cell Cycle / Actin Inhibitor |
| CR-1-31-b | exp474 (5nM) | Inhibits EIF4A, blocks translation by trapping EIF4A on mRNA at poly-purine sites | Class / Subclass 1: Proteostasis / Translation Inhibitor |
| Cyclic AMP | exp475 (200µM) | Second messenger, activates PKA, ion channels, cyclic nucleotide-binding proteins | Class / Subclass 1: Metabolism / Metabolite Class / Subclass 2: Signal Transduction / Kinase Activator |
| Dihydrosphingosine | exp476 (8µM) | Inhibits cytosolic phospholipase A2α (cPLA2α) activity | Class / Subclass 1: Metabolism / Metabolite |
| DKK1 | exp477 (89ng/mL) | Dickkopf1 (DKK1), recombinant protein inhibitor of WNT signaling, binds LRP5/LRP6 co-receptor and KRM1 | Class / Subclass 1: Signal Transduction / GPCR Antagonist |
| Doxorubicin | exp478 (20nM) | DNA intercalator, traps topoisomerase II complex | Class / Subclass 1: DNA Damage, Repair and Replication / Topoisomerase II Inhibitor Class / Subclass 2: Infectious Disease / Antibiotic |
| ETC-159 | exp480 (50µM) | Inhibits PORCN palmitoyl transferase that modifies WNT ligands | Class / Subclass 1: Signal Transduction / Other Inhibitor |
| Ethambutol | exp481 (25µM) | Inhibits arabinosyl transferase, interferes with cell wall formation | Class / Subclass 1: Infectious Disease / Antibiotic |
| Fas-L | exp482 (44ng/mL) | Ligand for Fas receptor, triggers apoptosis | Class / Subclass 1: Signal Transduction / Other Receptor Agonist |
| FTY720 | exp483 (3µM) | Agonist of sphingosine 1-phosphate receptor-1 (S1P1), derived from myriocin | Class / Subclass 1: Metabolism / Metabolic Enzyme Inhibitor |
| GSK-J5 | exp484 (1.5µM) | Inactive isomer of GSKJ4 | Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor |
| GSK 626616 | exp485 (14µM) | Inhibits DYRK3, prevents stress granule dissolution, mTORC1 release | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Heregulin B | exp486 (44ng/mL) | EGF family ligand for ErbB receptors, a.k.a. neuregulin-1 | Class / Subclass 1: Signal Transduction / Receptor Ligand |
| Hinokiflavone | exp487 (12µM) | Putative splicing inhibitor, ROS generation | Class / Subclass 1: Uncharacterized Mechanism / Natural Product Class / Subclass 2: Gene Regulation / Splicing Inhibitor |
| Hippuristanol | exp488 (120nM) exp489 (120nM) | Inhibits translation by trapping EIF4A on mRNA at poly-purine sites | Class / Subclass 1: Proteostasis / Translation Inhibitor |
| Hydroxychloroquine | exp490 (30µM) | Lysosomotropic agent, prevents sequestration of heme into hemozoin, forms toxic complex with heme, also inhibits TLR 7/9 | Class / Subclass 1: Infectious Disease / Antimalarial Class / Subclass 2: DNA Damage, Repair and Replication / Intercalating Agent Class / Subclass 3: Proteostasis / Autophagy Inhibitor |
| iCRT14 | exp492 (30µM) | Inhibits β-catenin-dependent transcription, may alter interaction of β-catenin with TCF4 | Class / Subclass 1: Gene Regulation / Transcription Inhibitor |
| IL-3 | exp493 (9ng/mL) | Ligand for IL3RA receptor, induces myeloid lineage proliferation and differentiation | Class / Subclass 1: Signal Transduction / Receptor Ligand |
| Isoniazid | exp494 (100µM) | Inhibits fatty acid synthases, pro-drug activated by catalase-peroxidase KatG | Class / Subclass 1: Infectious Disease / Antibiotic |
| IWR-1-endo | exp495 (50µM) | Stabilizes axin complex, inhibits Wnt/β-catenin signaling, also inhibits tankyrase | Class / Subclass 1: Signal Transduction / Other Inhibitor |
| Lead acetate | exp496 (990µM) exp497 (2000µM) exp498 (2000µM) | Industrial pollutant, heavy metal toxin | Class / Subclass 1: Environmental Stresses / Heavy Metal |
| LY2090314 | exp499 (3nM) exp500 (3nM) | Inhibits glycogen synthase kinase-3 (GSK-3), activates Wnt signalling | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Methotrexate | exp501 (10nM) | Inhibits dihydrofolate reductase (DHFR) | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor |
| Milciclib | exp502 (2µM) | Inhibits CDK2, also TRKA, CDK1, CDK4 | Class / Subclass 1: Cell Cycle / Cyclin Dependent Kinase Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Mitomycin C | exp503 (60nM) | DNA crosslinker, reductive activation forms a mitosene that N-alkylates successively DNA bases | Class / Subclass 1: DNA Damage, Repair and Replication / Inter/Intra-strand Crosslinker |
| MK2206 | exp504 (4µM) | Inhibit Akt1, Akt2, Akt3 | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| ML-792 | exp505 (200nM) | Inhibits SUMO-activating enzyme (SAE) | Class / Subclass 1: Proteostasis / SUMOylation Inhibitor |
| Momordin Ic | exp506 (10µM) | Triterpenoid saponin, putative SUMO-specific protease 1 (SENP1) inhibitor | Class / Subclass 1: Uncharacterized Mechanism / Traditional Medicine Class / Subclass 2: Proteostasis / SUMOylation Inhibitor |
| Monensin | exp507 (300nM) | Polyether antibiotic, binds monovalent cations, Na+/H+ antiporter, blocks Golgi transport | Class / Subclass 1: Infectious Disease / Antibiotic Class / Subclass 2: Organelle Function / Membrane Ionophore |
| N,N-Dimethylsphingosine | exp508 (2.5µM) | Inhibits sphingosine kinase, blocks sphingosine 1-phosphate (SPP) formation | Class / Subclass 1: Metabolism / Metabolite Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| Nicotine | exp510 (3000µM) | Agonist for nicotinic acetylcholine receptors (nAChRs) | Class / Subclass 1: Environmental Stresses / Psychoactive Drug Class / Subclass 2: Signal Transduction / Other Receptor Agonist |
| Olaparib | exp512 (4µM) | Inhibits PARP1 and PARP2, blocks ssDNA break repair, selectively toxic to BRCA1/2 negative cancers | Class / Subclass 1: DNA Damage, Repair and Replication / PARP Inhibitor |
| ONC212 | exp513 (150nM) | Inhibits mitochondrial CLPP protease, more potent derivative of TIC10/ONC201, possible agonist of GPR132 | Class / Subclass 1: Proteostasis / Protease Inhibitor Class / Subclass 2: Signal Transduction / GPCR Agonist |
| Phorbol 12-myristate 13-acetate | exp514 (570nM) | Activates PKC isoforms, potent tumour promoter | Class / Subclass 1: Signal Transduction / Kinase Activator |
| PU-H71 | exp515 (1µM) | Inhibits HSP90 | Class / Subclass 1: Proteostasis / Chaperone Inhibitor |
| Pyrazinamide | exp516 (100µM) | Inhibits growth of Mycobacterium tuberculosis in combination with isoniazid, ethambutanol and rifampicin, converted to active pyrazinamide by pyrazinamidase | Class / Subclass 1: Infectious Disease / Antibiotic |
| Quercetin | exp517 (20µM) | General kinase inhibitor, may inhibit NF-‘_B, anti-oxidant, putative senolytic | Class / Subclass 1: Signal Transduction / Kinase Inhibitor Class / Subclass 2: Gene Regulation / Transcription Inhibitor Class / Subclass 3: Uncharacterized Mechanism / Natural Product |
| RK-33 | exp518 (8µM) | Inhibits DDX3 RNA helicase, causes G1 arrest and apoptosis, broad spectrum anti-viral | Class / Subclass 1: Proteostasis / Translation Inhibitor Class / Subclass 2: Infectious Disease / Antiviral |
| RS-1 | exp519 (10µM) | Activates DNA binding by RAD51 | Class / Subclass 1: DNA Damage, Repair and Replication / Repair Protein Activator |
| Rucaparib | exp520 (6.5µM) | PARP1/2/3 inhibitor (Clovis), PARP1 mediates single-strand break repair, which can lead to replication-induced double strand breaks to form if not repaired; specifically target cancer with BRCA1, BRCA2 or PALB2 mutations; FDA granted an accelerated approval for use in cases of pretreated advanced ovarian cancer | Class / Subclass 1: DNA Damage, Repair and Replication / DNA Repair Inhibitor |
| Salinomycin | exp521 (3.5µM) | Potassium ionophore antibiotic, has activity against cancer stem cells | Class / Subclass 1: Organelle Function / Membrane Ionophore |
| Staurosporine | exp524 (20nM) | Inhibits many protein kinases including PKC, PKA, tyrosine kinases, CDKs, others | Class / Subclass 1: Signal Transduction / Kinase Inhibitor |
| Sulforaphane | exp525 (9µM) exp526 (9µM) | Organosulfur compound, found in cruciferous plants | Class / Subclass 1: Uncharacterized Mechanism / Natural Product |
| Tanespimycin | exp527 (14µM) | Inhibits HSP90, derivative of geldanamycin, a.k.a 17-AAG | Class / Subclass 1: Proteostasis / Chaperone Inhibitor Class / Subclass 2: Infectious Disease / Antibiotic |
| TGF-β1 | exp528 (44ng/mL) | Ligand for TGF-β1 receptor | Class / Subclass 1: Signal Transduction / Other Receptor Agonist |
| Thimerosal | exp529 (850nM) | Organomercury compound, antiseptic and antifungal, approved preservative in vaccines | Class / Subclass 1: Infectious Disease / Antifungal |
| Thioridazine | exp530 (5µM) | DRD2/4 selectivity, causes cardiac arrhythmia, also has antibiotic activity against M. tuberculosis | Class / Subclass 1: Signal Transduction / GPCR Antagonist |
| THZ1 | exp531 (60nM) | Inhibits CDK7, forms covalent adduct, blocks phosphorylation of the C-terminal domain of RNA polymerase II | Class / Subclass 1: Gene Regulation / Transcription Inhibitor Class / Subclass 2: Signal Transduction / Kinase Inhibitor |
| TIC10 | exp532 (10µM) | Inhibits mitochondrial CLPP protease, a.k.a. ONC201, parent of ONC212, possible agonist of GPR132 | Class / Subclass 1: Proteostasis / Protease Inhibitor Class / Subclass 2: Signal Transduction / GPCR Agonist |
| TNF-α | exp533 (44ng/mL) | Ligand for TNFR1, induces apoptosis or necrosis | Class / Subclass 1: Signal Transduction / Other Receptor Agonist |
| Trientine | exp534 (500µM) | Copper-selective chelator, enhances renal excretion of copper | Class / Subclass 1: Environmental Stresses / Metal Chelator |
| Trimetrexate | exp535 (30nM) | Inhibits bacterial, protozoan, and mammalian dihydrofolate reductase (DHFR), methotrexate analog | Class / Subclass 1: Metabolism / Antimetabolite Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor Class / Subclass 3: Infectious Disease / Antibiotic |
| Vitamin D3 | exp536 (40µM) | Steroid hormone, converted to active 1,25-dihydroxycholecalciferol (calcitriol), role in calcium homeostasis | Class / Subclass 1: Metabolism / Vitamin Class / Subclass 2: Metabolism / Metabolite Class / Subclass 3: SIgnal Transduction / Receptor Ligand |
| WNT3A | exp537 (44ng/mL) | Ligand for Frizzled receptor complex, stabilizes ‘_-catenin, induces TCS/LEF-dependent transcription | Class / Subclass 1: Signal Transduction / GPCR Agonist |
| ZLN024 | exp538 (50µM) | Activates AMPK, allosteric | Class / Subclass 1: Signal Transduction / Kinase Activator |
| Hypoxia 5% O2 | exp191 | Reduced growth oxygen | Class / Subclass 1: Environmental Stresses / Stress Condition |
| 35°C | exp302 | Reduced growth temperature | Class / Subclass 1: Environmental Stresses / Stress Condition |
| 39°C | exp303 | Elevated growth temperature | Class / Subclass 1: Environmental Stresses / Stress Condition |
| FBS Sub-Optimal Growth | exp426 (10%) | Unknown, poor batch of FBS | Class / Subclass 1: Environmental Stresses / Toxin |
| 42°C | exp539 | Elevated growth temperature | Class / Subclass 1: Environmental Stresses / Stress Condition |