====== GSK-LSD1 10μM R03 exp123 ====== ==== Mechanism of Action ==== Inhibits LSD1 histone demethylase (H3K4me/me2, H3K9me) * **Class / Subclass 1:** Gene Regulation / Epigenetic Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%GSK-LSD1 Dihydrochloride%% * **Synonyms:** N/A * **CAS #:** N/A * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/91663353|91663353]] * **IUPAC:** %%N-[(1R,2S)-2-phenylcyclopropyl]piperidin-4-amine;dihydrochloride%% * **INCHI Name:** InChI=1S/C14H20N2.2ClH/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12;;/h1-5,12-16H,6-10H2;2*1H/t13-,14+;;/m0../s1 * **INCHI Key:** PJFZOGMSPBHPNS-WICJZZOFSA-N * **Molecular Weight:** 289.2 * **Canonical SMILES:** C1CNCCC1NC2CC2C3=CC=CC=C3.Cl.Cl * **Isomeric SMILES:** C1CNCCC1N[C@@H]2C[C@H]2C3=CC=CC=C3.Cl.Cl * **Molecular Formula:** C14H22Cl2N2 {{:chemogenomics:structures:chem-0076.svg?nolink}} * **Supplier Name:** Tocris Bioscience * **Catalog #:** 5361 * **Lot #:** N/A * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C14H20N2 217.16993; found 217.16937 * **Platform ID:** GSK-LSD1 * **Min:** -4.3978; **Max:** 8.0909 {{:chemogenomics:dose_response:dr_81.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |N/A | | IC30 |N/A | | IC40 |N/A | | IC50 |N/A | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 03 * **Dose**: 10µM * **Days of incubation**: 8 * **Doublings**: 7.9 * **Numbers of reads**: 10549262 ==== Screen Results ==== ^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^ |0/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/GSK-LSD1_10uM_Round-3_exp123.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp123.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SLC6A12|SLC6A12]]|-2.56|0.18| |[[:human_genes:N:NPPA|NPPA]]|-2.50|0.18| |[[:human_genes:P:PEBP4|PEBP4]]|-2.27|0.49| |[[:human_genes:D:DPAGT1|DPAGT1]]|-2.27|0.82| |[[:human_genes:W:WDR60|WDR60]]|-2.24|0.82| |[[:human_genes:S:SLC4A7|SLC4A7]]|-2.17|0.82| |[[:human_genes:F:FAM231B|FAM231B]]|-2.14|0.82| |[[:human_genes:H:HGC6.3|HGC6.3]]|-2.08|0.89| |[[:human_genes:H:HPSE|HPSE]]|-2.03|0.82| |[[:human_genes:N:NCBP1|NCBP1]]|-2.03|0.89| |[[:human_genes:Z:ZNF343|ZNF343]]|-2.02|0.89| |[[:human_genes:P:PRRG2|PRRG2]]|-2.02|0.82| |[[:human_genes:S:SAE1|SAE1]]|-2.00|0.89| |[[:human_genes:G:GATM|GATM]]|-1.99|0.89| |[[:human_genes:F:FFAR1|FFAR1]]|-1.98|0.82| |[[:human_genes:H:HABP4|HABP4]]|-1.97|0.82| |[[:human_genes:S:SEPSECS|SEPSECS]]|-1.97|0.89| |[[:human_genes:R:R3HCC1|R3HCC1]]|-1.97|0.89| |[[:human_genes:S:STARD8|STARD8]]|-1.96|0.82| |[[:human_genes:S:SRD5A1|SRD5A1]]|-1.95|0.82| |[[:human_genes:A:AFF2|AFF2]]|-1.94|0.82| |[[:human_genes:X:XCR1|XCR1]]|-1.90|0.82| |[[:human_genes:T:TMEM179B|TMEM179B]]|-1.87|0.82| |[[:human_genes:A:ATG9A|ATG9A]]|-1.86|0.82| |[[:human_genes:I:ID3|ID3]]|-1.85|0.82| |[[:human_genes:D:DCUN1D1|DCUN1D1]]|-1.84|0.82| |[[:human_genes:G:GCM2|GCM2]]|-1.84|0.89| |[[:human_genes:U:UBE3A|UBE3A]]|-1.84|0.82| |[[:human_genes:I:INSR|INSR]]|-1.83|0.82| |[[:human_genes:G:GCLC|GCLC]]|-1.83|0.89| |[[:human_genes:G:GDF9|GDF9]]|1.99|0.81| |[[:human_genes:C:CNOT3|CNOT3]]|2.02|0.81| |[[:human_genes:S:SRSF3|SRSF3]]|2.02|0.66| |[[:human_genes:C:COLCA2|COLCA2]]|2.03|0.81| |[[:human_genes:C:CDK1|CDK1]]|2.04|0.85| |[[:human_genes:M:MANBA|MANBA]]|2.05|0.64| |[[:human_genes:A:ASPHD2|ASPHD2]]|2.06|0.40| |[[:human_genes:G:GPNMB|GPNMB]]|2.08|0.81| |[[:human_genes:C:CNTN1|CNTN1]]|2.08|0.40| |[[:human_genes:T:TOPBP1|TOPBP1]]|2.10|0.81| |[[:human_genes:A:ATRNL1|ATRNL1]]|2.10|0.40| |[[:human_genes:T:TBC1D3I|TBC1D3I]]|2.12|0.85| |[[:human_genes:T:TBC1D3E|TBC1D3E]]|2.12|0.85| |[[:human_genes:T:TBC1D3K|TBC1D3K]]|2.13|0.85| |[[:human_genes:T:TBC1D3L|TBC1D3L]]|2.13|0.85| |[[:human_genes:E:EOMES|EOMES]]|2.14|0.40| |[[:human_genes:E:EIF3J|EIF3J]]|2.14|0.85| |[[:human_genes:G:G3BP1|G3BP1]]|2.15|0.40| |[[:human_genes:S:ST5|ST5]]|2.15|0.45| |[[:human_genes:C:CDT1|CDT1]]|2.18|0.81| |[[:human_genes:P:PLN|PLN]]|2.19|0.85| |[[:human_genes:R:RNF165|RNF165]]|2.19|0.40| |[[:human_genes:E:ENPP4|ENPP4]]|2.19|0.40| |[[:human_genes:B:B3GALNT2|B3GALNT2]]|2.25|0.40| |[[:human_genes:P:PIWIL3|PIWIL3]]|2.26|0.40| |[[:human_genes:K:KIF4A|KIF4A]]|2.32|0.28| |[[:human_genes:F:FOLR1|FOLR1]]|2.32|0.28| |[[:human_genes:T:TBC1D3C|TBC1D3C]]|2.33|0.28| |[[:human_genes:S:SST|SST]]|2.34|0.28| |[[:human_genes:R:RARS|RARS]]|2.37|0.85| No correlation data above threshold. (correlation > 0.05) No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)