ZM336372 [Ligand Id: 9130] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL186526 (ZM-336372)
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase 11/MAP kinase p38 beta in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
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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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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of SAPK2a/p38-alpha B 5.7 pIC50 2000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Concentration required to inhibit human mitogen activated protein kinase p38 activity B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2004) 14: 5383-5387 [PMID:15454231]
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL Inhibition of SAPK2b/p38beta B 5.7 pIC50 2000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 in the presence of 100uM ATP B 6.64 pIC50 230 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of protein kinase c-raf B 4.77 pIC50 17000 nM IC50 Bioorg Med Chem Lett (2004) 14: 5383-5387 [PMID:15454231]
ChEMBL Inhibition of Raf1 kinase B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2008) 18: 2346-2350 [PMID:18346893]
ChEMBL Inhibition of cRAF1 B 7.15 pIC50 70 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of c-Raf kinase B 7.15 pIC50 70 nM IC50 Nat Chem Biol (2006) 2: 358-364 [PMID:16783341]
ChEMBL Inhibition of c-Raf in the presence of 100uM ATP B 7.51 pIC50 31 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
GtoPdb - - 7.51 pIC50 31 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363];
Biochem J (2003) 371: 199-204 [PMID:12534346]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Inhibition of RIP2 in the presence of 100uM ATP B 4 pIC50 >100000 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
ChEMBL Inhibition of Lck in the presence of 50uM ATP B 6.24 pIC50 570 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]

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]