cobimetinib [Ligand Id: 7626] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2146883 (RG7420, RG 7420, RG-7420, Gdc-0623, Rg-7421, Rg-7420, Cotellic, Cobimetinib, GDC-0973, XL-518)
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
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  • mitogen-activated protein kinase kinase 2 in Human [GtoPdb: 2063] [UniProtKB: P36507]
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  • mitogen-activated protein kinase kinase 7 in Human [GtoPdb: 2068] [UniProtKB: O14733]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Inhibition of MEK1 (unknown origin) B 8.38 pIC50 4.2 nM IC50 Drug Metab. Dispos. (2012) 40: 919-927 [PMID:22315332]
ChEMBL Inhibition of MEK1-mediated ERK2 T202/Y204 phosphorylation using biotinylated MBP as substrate preincubated for 30 mins measured after 100 mins by cRAF-MEK-ERK enzyme coupled assay B 9.05 pIC50 0.9 nM IC50 ACS Med. Chem. Lett. (2012) 3: 416-421 [PMID:24900486]
GtoPdb Biochemical assay measuring MEK-induced phosphorylation of ERK residues T202 and Y204. - 9.05 pIC50 0.9 nM IC50 ACS Med Chem Lett (2012) 3: 416-21 [PMID:24900486]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Inhibition of B-raf V600E mutant in human COLO205 cells assessed as reduction of ERK1/ERK2 phosphorylation B 8.74 pIC50 1.8 nM IC50 Drug Metab. Dispos. (2012) 40: 919-927 [PMID:22315332]
mitogen-activated protein kinase kinase 2 in Human [GtoPdb: 2063] [UniProtKB: P36507]
GtoPdb - - 6.7 pIC50 199 nM IC50 ACS Med Chem Lett (2012) 3: 416-21 [PMID:24900486]
mitogen-activated protein kinase kinase 7 in Human [GtoPdb: 2068] [UniProtKB: O14733]
GtoPdb - - 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2012) 3: 416-21 [PMID:24900486]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]