romaciclib [Ligand Id: 13753] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4225966 (Sel-120 free base) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 8/CDK8/Cyclin C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038474] [GtoPdb: 1980] [UniProtKB: P24863, P49336] | ||||||||
| GtoPdb | Binding dissociation constant for hCDK8 protein | - | 8.52 | pKd | 3 | nM | Kd | Oncotarget (2017) 8: 33779-33795 [PMID:28422713] |
| ChEMBL | Inhibition of His tagged human recombinant CDK8/Cyclin C expressed in baculovirus expression system incubated for 15 mins by FRET-based LanthaScreen binding competition assay | B | 7.85 | pIC50 | 14.11 | nM | IC50 | J Med Chem (2023) 66: 5439-5452 [PMID:37029334] |
| ChEMBL | Inhibition of CDK8/Cyclin C (unknown origin) | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (2022) 65: 6390-6418 [PMID:35485642] |
| GtoPdb | Inhibition of CDK8/CycC kinase activity | - | 8.36 | pIC50 | 4.4 | nM | IC50 | Oncotarget (2017) 8: 33779-33795 [PMID:28422713] |
| ChEMBL | Inhibition of CDK8/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by radiometric method | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2018) 61: 5073-5092 [PMID:29266937] |
| cyclin dependent kinase 8/Cell division protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336] | ||||||||
| GtoPdb | Binding dissociation constant for hCDK8 protein | - | 8.52 | pKd | 3 | nM | Kd | Oncotarget (2017) 8: 33779-33795 [PMID:28422713] |
| ChEMBL | Inhibition of CDK8 (unknown origin) in presence of ATP by ADP-Glo assay | B | 7.43 | pIC50 | 37.2 | nM | IC50 | Eur J Med Chem (2023) 251: 115214-115214 [PMID:36889252] |
| ChEMBL | Inhibition of CDK8 (unknown origin) | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525] |
| GtoPdb | Inhibition of CDK8/CycC kinase activity | - | 8.36 | pIC50 | 4.4 | nM | IC50 | Oncotarget (2017) 8: 33779-33795 [PMID:28422713] |
| cyclin dependent kinase 19/Cyclin-C/Cyclin-dependent kinase 19 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883323] [GtoPdb: 1972] [UniProtKB: P24863, Q9BWU1] | ||||||||
| GtoPdb | Inhibition of CDK19/CycC kinase activity | - | 7.98 | pIC50 | 10.4 | nM | IC50 | Oncotarget (2017) 8: 33779-33795 [PMID:28422713] |
| ChEMBL | Inhibition of CDK19/Cyclin C (unknown origin) | B | 7.98 | pIC50 | 10.4 | nM | IC50 | J Med Chem (2022) 65: 6390-6418 [PMID:35485642] |
| ChEMBL | Inhibition of CDK19/Cyclin C (unknown origin) | B | 7.98 | pIC50 | 10.4 | nM | IC50 | Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525] |
| ChEMBL | Inhibition of CDK19/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by radiometric method | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2018) 61: 5073-5092 [PMID:29266937] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Inhibition of CDK9 (unknown origin) in presence of [gamma33P]ATP by radiometric method | B | 5.97 | pIC50 | 1070 | nM | IC50 | J Med Chem (2018) 61: 5073-5092 [PMID:29266937] |
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]
