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]
Created with Highcharts 10.3.3ValuesChart context menuc-Jun N-terminal kinase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuInhibitor of nuclear factor kappa B kinase beta subunitpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase ERK1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase p38 alphapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • mitogen-activated protein kinase 11/MAP kinase p38 beta in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase p38 betapKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • mitogen-activated protein kinase 13/MAP kinase p38 delta in Human [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase p38 deltapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase 12/MAP kinase p38 gamma in Human [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase p38 gammapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
Created with Highcharts 10.3.3ValuesChart context menuMitogen-activated protein kinase kinase kinase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 in Human [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase c-TAK1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
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 35:

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]