istisociclib [Ligand Id: 13068] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5199065 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 12/CDK12/Cyclin K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106169] [GtoPdb: 1965] [UniProtKB: O75909, Q9NYV4] | ||||||||
| ChEMBL | Inhibition of human CDK12/Cyclin K preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 30 uM ATP | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 17/CDK17/Cyclin-Y in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523637] [GtoPdb: 1970] [UniProtKB: Q00537, Q8ND76] | ||||||||
| ChEMBL | Inhibition of human CDK17/Cyclin Y preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 20 uM ATP | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 18/CDK18/Cyclin Y in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106161] [GtoPdb: 1971] [UniProtKB: Q07002, Q8ND76] | ||||||||
| ChEMBL | Inhibition of human CDK18/Cyclin Y preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 20 uM ATP | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 1/CDK1/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038467] [GtoPdb: 1961] [UniProtKB: P06493, P20248] | ||||||||
| ChEMBL | Inhibition of human CDK1/Cyclin A preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.53 | pIC50 | 2980 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 2/CDK2/Cyclin A1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038470] [GtoPdb: 1973] [UniProtKB: P24941, P78396] | ||||||||
| GtoPdb | Inhibition of CDK2/Cyclin A | - | 6.4 | pIC50 | 397 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of human CDK2/Cyclin A preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 6.4 | pIC50 | 397 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 3/CDK3/Cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038471] [GtoPdb: 1975] [UniProtKB: P24864, Q00526] | ||||||||
| ChEMBL | Inhibition of human CDK3/Cyclin E preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 100 uM ATP | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of human CDK3/Cyclin E preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.85 | pIC50 | 1420 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385, Q00534] | ||||||||
| ChEMBL | Inhibition of human CDK6/Cyclin D1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 100 uM ATP | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of human CDK6/Cyclin D1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.4 | pIC50 | 3950 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 8/CDK8/Cyclin C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038474] [GtoPdb: 1980] [UniProtKB: P24863, P49336] | ||||||||
| ChEMBL | Inhibition of human CDK8/Cyclin C preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| GtoPdb | Inhibition of CDK9/Cyclin T1 | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of CDK9/Cyclin T1 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2022) 65: 6390-6418 [PMID:35485642] |
| ChEMBL | Inhibition of human CDK9/Cyclin T1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 19/Cell division cycle 2-like protein kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6002] [GtoPdb: 1972] [UniProtKB: Q9BWU1] | ||||||||
| ChEMBL | Inhibition of CDK19 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 8/Cell division protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336] | ||||||||
| ChEMBL | Inhibition of CDK8 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 19/Cyclin-C/Cyclin-dependent kinase 19 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883323] [GtoPdb: 1972] [UniProtKB: P24863, Q9BWU1] | ||||||||
| ChEMBL | Inhibition of human CDK19/Cyclin C preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 20 uM ATP | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Inhibition of CDK12 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 6.23 | pIC50 | 588 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] | ||||||||
| ChEMBL | Inhibition of CDK13 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 6.43 | pIC50 | 372 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13/Cyclin-K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296067] [GtoPdb: 1966] [UniProtKB: O75909, Q14004] | ||||||||
| ChEMBL | Inhibition of human CDK13/Cyclin K preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 5 uM ATP | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 14/Cyclin-dependent kinase 14/Cyclin-Y in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296115] [GtoPdb: 1967] [UniProtKB: O94921, Q8ND76] | ||||||||
| ChEMBL | Inhibition of human CDK14/Cyclin Y preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 15 uM ATP | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| GtoPdb | Inhibition of CDK2/Cyclin A | - | 6.4 | pIC50 | 397 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of CDK2 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 6.4 | pIC50 | 396 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] | ||||||||
| ChEMBL | Inhibition of CDK3 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Inhibition of CDK4 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibition of human CDK4/Cyclin D1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 100 uM ATP | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of human CDK4/Cyclin D1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.5 | pIC50 | 3130 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of CDK5 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of human CDK5/P25 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.74 | pIC50 | 1820 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
| ChEMBL | Inhibition of CDK6 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Inhibition of CDK7 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613, P51946] | ||||||||
| ChEMBL | Inhibition of human CDK7/Cyclin H preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs in presence of 50 uM ATP | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of human CDK7/Cyclin H preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs | B | 5.82 | pIC50 | 1510 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| GtoPdb | Inhibition of CDK9/Cyclin T1 | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2023) 66: 15629-15647 [PMID:37967851] |
| ChEMBL | Inhibition of CDK9 (unknown origin) by hotspot kinase assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2022) 65: 6356-6389 [PMID:35235745] |
| ChEMBL | Inhibition of CDK9 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 8.22 | pIC50 | 6 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 16/Serine/threonine-protein kinase PCTAIRE-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Inhibition of CDK16 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 17/Serine/threonine-protein kinase PCTAIRE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] | ||||||||
| ChEMBL | Inhibition of CDK17 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 18/Serine/threonine-protein kinase PCTAIRE-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5316] [GtoPdb: 1971] [UniProtKB: Q07002] | ||||||||
| ChEMBL | Inhibition of CDK18 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| cyclin dependent kinase 14/Serine/threonine-protein kinase PFTAIRE-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6162] [GtoPdb: 1967] [UniProtKB: O94921] | ||||||||
| ChEMBL | Inhibition of CDK14 (unknown origin) incubated for 120 mins in presence of ATP by HotSpot kinase assay | B | 5.92 | pIC50 | >1200 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
