zemirciclib [Ligand Id: 11782] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4462530 (Azd 4573, Azd-4573, Azd4573, AZD-4573, AZD4573) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Inhibition of CK1gamma1 (unknown origin) in presence of 5 mM ATP | B | 5.26 | pIC50 | 5520 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| casein kinase 1 gamma 2/Casein kinase I gamma 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Inhibition of CK1gamma2 (unknown origin) in presence of 5 mM ATP | B | 5.18 | pIC50 | 6660 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 12/CDK12/Cyclin K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106169] [GtoPdb: 1965] [UniProtKB: O75909, Q9NYV4] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal GST-TEV tagged CDK12 (696 to 1082 residues)/full length human CyclinK expressed in baculovirus expression system using FITC-X-GSRTPMY-NH2 as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 240 mins in presence of 5 mM ATP by mobility shift assay | B | 5.09 | pIC50 | 8070 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948] | ||||||||
| ChEMBL | Inhibition of recombinant full length human CDK7/cyclinH1/MAT1 expressed in insect cells using 5FAM-YSPTSPSYSPTSPSYSPTSPSKKKK-NH2 as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 120 mins in presence of 5 mM ATP by mobility shift assay | B | 5.86 | pIC50 | 1370 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Binding affinity to human CDK9/CyclinT assessed as equilibrium dissociation constant by surface plasmon resonance analysis | B | 10.05 | pKd | 0.09 | nM | Kd | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of recombinant full length human N-terminal GST-fused CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus infected insect cells using FITC-X-GSRTPMY-NH2 as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 90 mins in presence of 5 mM ATP by mobility shift assay | B | 8.4 | pIC50 | <4 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of full length human CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus expression system in presence of high ATP | B | 8.4 | pIC50 | <4 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| ChEMBL | Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay | B | 8.4 | pIC50 | <4 | nM | IC50 | J Med Chem (2022) 65: 6390-6418 [PMID:35485642] |
| GtoPdb | Inhibition of CDK9 activity in a biochemical enzyme assay | - | 8.4 | pIC50 | <4 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of full length human CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus expression system in presence of Km ATP | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Inhibition of JNK1 (unknown origin) in presence of 5 mM ATP | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 in human MCF7 cells assessed as reduction in PP1alpha phosphorylation at T320 residue incubated for 6 hrs by immunoblot analysis | B | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of recombinant full length human His-tagged CDK1/CyclinB expressed in baculovirus infected insect cells using 5FAM-RRRFRPASPLRGPPKCOOH as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 90 mins in presence of 5 mM ATP by mobility shift assay | B | 6.93 | pIC50 | 117 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 in human MCF7 cells assessed as reduction in Rb phosphorylation at T821 residue incubated for 6 hrs by immunoblot analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of recombinant full length human CDK2/CyclinE expressed in insect cells using FL-Ahx-QSPKKG-CONH2 as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 90 mins in presence of 5 mM ATP by mobility shift assay | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| 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) in presence of 5 mM ATP | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| 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) in presence of 5 mM ATP | B | 6.3 | pIC50 | 499 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| 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) in presence of 5 mM ATP | B | 5.9 | pIC50 | 1270 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| 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) in presence of 5 mM ATP | B | 6.44 | pIC50 | 363 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Inhibition of CDK7 in human MCF7 cells assessed as RNA polymerase2 phosphorylation at serine 5 residue residue incubated for 6 hrs by immunoblot analysis | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Reversible inhibition of CDK9 in human MCF7 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser2 residues preincubated for 6 hrs followed by compound washout and measured after 2 hrs by immunofluorescence assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of CDK9 in human MCF7 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser2 residues measured after 6 hrs by immunofluorescence assay | B | 7.87 | pIC50 | 13.4 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 8.4 | pIC50 | <4 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 8.4 | pIC50 | <4 | nM | IC50 | Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525] |
| GtoPdb | Inhibition of CDK9 activity in a biochemical enzyme assay | - | 8.4 | pIC50 | <4 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| ChEMBL | Inhibition of CDK9 in human MV4-11 cells assessed as induction of caspase-3/7 activation measured after 6 hrs followed by Caspase-glo reagent based assay | B | 7.86 | pEC50 | 13.7 | nM | EC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630] | ||||||||
| ChEMBL | Inhibition of DYRK2 (unknown origin) in presence of 5 mM ATP | B | 5.06 | pIC50 | 8620 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Inhibition of GSK3alpha (unknown origin) in presence of 5 mM ATP | B | 6.73 | pIC50 | 187 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3beta (unknown origin) in presence of 5 mM ATP | B | 6.61 | pIC50 | 247 | nM | IC50 | J Med Chem (2020) 63: 15564-15590 [PMID:33306391] |
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]
