TAK-715 [Ligand Id: 9328] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL363648 (Tak-715, TAK 715, TAK-715)
  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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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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  • mitogen-activated protein kinase 13/MAP kinase p38 delta in Human [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
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  • mitogen-activated protein kinase 12/MAP kinase p38 gamma in Human [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
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  • mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
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  • microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 in Human [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibitory concentration against c-Jun N-terminal kinase 1 B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibitory concentration against I-kappa-B kinase beta B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibitory concentration against mitogen-activated protein kinase 3 B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate preincubated for 5 mins followed by ATP addition measured after 20 mins by TR-FRET assay B 6.62 pIC50 240 nM IC50 Bioorg Med Chem (2018) 26: 647-660 [PMID:29291937]
ChEMBL Displacement of SKF86002 from recombinant human p38alpha by fluorescence-based assay B 7.15 pIC50 71 nM IC50 Medchemcomm (2013) 4: 371-377
ChEMBL In vitro inhibitory activity against mitogen-activated protein kinase p38 alpha B 8.15 pIC50 7.1 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
ChEMBL Inhibition of p38 alpha (unknown origin) B 8.15 pIC50 7.1 nM IC50 Eur J Med Chem (2021) 215: 113277-113277 [PMID:33601311]
GtoPdb - - 8.15 pIC50 7.1 nM IC50 J Med Chem (2005) 48: 5966-79 [PMID:16162000]
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL Inhibitory concentration against mitogen-activated protein kinase p38-beta B 6.7 pIC50 200 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
GtoPdb - - 6.7 pIC50 200 nM IC50 J Med Chem (2005) 48: 5966-79 [PMID:16162000]
mitogen-activated protein kinase 13/MAP kinase p38 delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
ChEMBL Inhibitory concentration against mitogen-activated protein kinase p38-delta B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
mitogen-activated protein kinase 12/MAP kinase p38 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
ChEMBL Inhibitory concentration against mitogen-activated protein kinase p38-gamma B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
ChEMBL Inhibitory concentration against Mitogen-activated protein kinase kinase kinase 1 (MEKK1) B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]
microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
ChEMBL Inhibitory concentration against Mitogen-activated protein kinase kinase kinase 7 (TAK1) B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 5966-5979 [PMID:16162000]

ChEMBL data shown on this page come from version 32:

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]