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ChEMBL ligand: CHEMBL4277900 (Crozbaciclib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 1/CDK1/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038467] [GtoPdb: 1961] [UniProtKB: P06493, P20248] | ||||||||
ChEMBL | Inhibition of CDK1/Cyclin-A2 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay | B | 5.57 | pIC50 | 2707 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] | ||||||||
GtoPdb | Inhibition of CDK6/cyclin D3 in vitro | - | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
ChEMBL | Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
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 CDK2/Cyclin-E1 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay | B | 5.63 | pIC50 | 2321 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
GtoPdb | Inhibition of CDK4/cyclin D1 in vitro | - | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
ChEMBL | Inhibition of CDK4/Cyclin-D1 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
mitogen-activated protein kinase kinase kinase 14/Mitogen-activated protein kinase kinase kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5888] [GtoPdb: 2074] [UniProtKB: Q99558] | ||||||||
ChEMBL | Inhibition of recombinant human GST-tagged NIK expressed in baculovirus expression system using ser/thr-7 as substrate preincubated for 15 mins followed by ATP addition measured after 60 mins | B | 7.35 | pIC50 | 45 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of recombinant human GST-tagged JAK3 cytoplasmic domain (781 to 1124 residues) expressed in baculovirus expression system using ULight-JAK-1 peptide as substrate preincubated for 15 mins followed by ATP addition measured after 90 mins | B | 6.81 | pIC50 | 154 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
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]