====== A-196 10μM R03 exp114 ====== ==== Mechanism of Action ==== Inhibits SUV420H1 and SUV420H2 inhibitor, blocks di/trimethylation of H4K20me * **Class / Subclass 1:** Gene Regulation / Epigenetic Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%6,7-Dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine%% * **Synonyms:** N/A * **CAS #:** 1982372-88-2 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/117072548|117072548]] * **IUPAC:** %%6,7-dichloro-N-cyclopentyl-4-pyridin-4-ylphthalazin-1-amine%% * **INCHI Name:** InChI=1S/C18H16Cl2N4/c19-15-9-13-14(10-16(15)20)18(22-12-3-1-2-4-12)24-23-17(13)11-5-7-21-8-6-11/h5-10,12H,1-4H2,(H,22,24) * **INCHI Key:** ABGOSOMRWSYAOB-UHFFFAOYSA-N * **Molecular Weight:** 359.2 * **Canonical SMILES:** C1CCC(C1)NC2=NN=C(C3=CC(=C(C=C32)Cl)Cl)C4=CC=NC=C4 * **Isomeric SMILES:** N/A * **Molecular Formula:** C18H16Cl2N4 {{:chemogenomics:structures:chem-0070.svg?nolink}} * **Supplier Name:** Structural Genomics Consortium * **Catalog #:** N/A * **Lot #:** N/A * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C18H16Cl2N4 359.08248; found 359.08319 * **Platform ID:** A-196 * **Min:** 0.0245; **Max:** 32.4348 {{:chemogenomics:dose_response:dr_62.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |11.6475 | | 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**: 7.5 * **Numbers of reads**: 10046263 ==== 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^ |4/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/A-196_10uM_Round-3_exp114.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp114.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SLC5A3|SLC5A3]]|-3.90|<0.01| |[[:human_genes:S:SLC7A5|SLC7A5]]|-3.17|<0.01| |[[:human_genes:A:ALG13|ALG13]]|-2.90|0.03| |[[:human_genes:F:FLVCR1|FLVCR1]]|-2.84|0.02| |[[:human_genes:D:DPAGT1|DPAGT1]]|-2.53|0.22| |[[:human_genes:K:KCNC3|KCNC3]]|-2.46|0.14| |[[:human_genes:S:SLC52A2|SLC52A2]]|-2.44|0.11| |[[:human_genes:E:ENO1|ENO1]]|-2.41|0.21| |[[:human_genes:F:FAM122A|FAM122A]]|-2.37|0.13| |[[:human_genes:C:CHKA|CHKA]]|-2.36|0.13| |[[:human_genes:G:GCLC|GCLC]]|-2.29|0.21| |[[:human_genes:C:COL21A1|COL21A1]]|-2.28|0.21| |[[:human_genes:S:SYS1|SYS1]]|-2.27|0.28| |[[:human_genes:K:KIAA0020|KIAA0020]]|-2.27|0.28| |[[:human_genes:M:MRPL4|MRPL4]]|-2.24|0.21| |[[:human_genes:D:DMRTA2|DMRTA2]]|-2.23|0.21| |[[:human_genes:K:KRTAP10-4|KRTAP10-4]]|-2.22|0.44| |[[:human_genes:C:C6orf136|C6orf136]]|-2.21|0.21| |[[:human_genes:E:ERVFRD-1|ERVFRD-1]]|-2.14|0.21| |[[:human_genes:A:ALAD|ALAD]]|-2.13|0.28| |[[:human_genes:S:SLC31A2|SLC31A2]]|-2.13|0.21| |[[:human_genes:S:SNF8|SNF8]]|-2.13|0.28| |[[:human_genes:P:PTPRN2|PTPRN2]]|-2.11|0.21| |[[:human_genes:H:HMGCS2|HMGCS2]]|-2.10|0.21| |[[:human_genes:V:VMO1|VMO1]]|-2.10|0.21| |[[:human_genes:U:UHRF1|UHRF1]]|-2.06|0.34| |[[:human_genes:P:PIK3CD|PIK3CD]]|-2.04|0.36| |[[:human_genes:B:BOLA3|BOLA3]]|-2.00|0.28| |[[:human_genes:A:ARID4B|ARID4B]]|-1.97|0.44| |[[:human_genes:P:PCDHB11|PCDHB11]]|-1.97|0.32| |[[:human_genes:E:EXOSC8|EXOSC8]]|2.00|0.48| |[[:human_genes:Z:ZDHHC2|ZDHHC2]]|2.04|0.43| |[[:human_genes:G:GPR19|GPR19]]|2.04|0.43| |[[:human_genes:F:FLI1|FLI1]]|2.06|0.43| |[[:human_genes:N:NUP88|NUP88]]|2.07|0.55| |[[:human_genes:B:BCL2A1|BCL2A1]]|2.08|0.43| |[[:human_genes:S:SLC8B1|SLC8B1]]|2.09|0.43| |[[:human_genes:R:RPL18|RPL18]]|2.09|0.76| |[[:human_genes:S:SART3|SART3]]|2.09|0.60| |[[:human_genes:D:DIEXF|DIEXF]]|2.09|0.43| |[[:human_genes:O:OR51E2|OR51E2]]|2.10|0.43| |[[:human_genes:I:ISCU|ISCU]]|2.11|0.76| |[[:human_genes:O:OGDH|OGDH]]|2.11|0.51| |[[:human_genes:F:FAM217A|FAM217A]]|2.12|0.43| |[[:human_genes:M:MASTL|MASTL]]|2.12|0.60| |[[:human_genes:B:BRCA1|BRCA1]]|2.14|0.43| |[[:human_genes:V:VPRBP|VPRBP]]|2.15|0.59| |[[:human_genes:R:ROBO1|ROBO1]]|2.17|0.43| |[[:human_genes:C:CRYBB1|CRYBB1]]|2.19|0.43| |[[:human_genes:N:NUP160|NUP160]]|2.24|0.43| |[[:human_genes:P:POLD3|POLD3]]|2.27|0.70| |[[:human_genes:L:LUC7L3|LUC7L3]]|2.28|0.51| |[[:human_genes:P:PCDHGA9|PCDHGA9]]|2.30|0.42| |[[:human_genes:U:UTP20|UTP20]]|2.32|0.48| |[[:human_genes:Z:ZNF852|ZNF852]]|2.41|0.43| |[[:human_genes:O:OR10H4|OR10H4]]|2.41|0.34| |[[:human_genes:P:PATZ1|PATZ1]]|2.43|0.43| |[[:human_genes:C:CFAP45|CFAP45]]|2.51|0.52| |[[:human_genes:T:TMEM184C|TMEM184C]]|2.67|0.34| |[[:human_genes:D:DNM2|DNM2]]|2.68|0.59| ^Screen^Correlation^Plot^ |[[:results:exp149|SB203580 25μM R03 exp149]]|0.071|| {{:chemogenomics:comparison_plots:exp114_vs_exp149.png?nolink |}} No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)