crozbaciclib [Ligand Id: 12076] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
