pamapimod [Ligand Id: 9915] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1090089 (Pamapimod, R1503, R-1503, Ro-4402257, RO 4402257)
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • coenzyme Q8A/Chaperone activity of bc1 complex-like, mitochondrial in Human [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60]
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  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
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  • mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
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  • discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
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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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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha 4 in Human [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
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  • serine/threonine kinase 36/Serine/threonine-protein kinase 36 in Human [ChEMBL: CHEMBL4312] [GtoPdb: 2223] [UniProtKB: Q9NRP7]
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  • cyclin G associated kinase/Serine/threonine-protein kinase GAK in Human [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976]
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  • nemo like kinase/Serine/threonine protein kinase NLK in Human [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Binding affinity to CSNK1epsilon B 6.59 pKd 260 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of CSNK1epsilon B 6.59 pKd 260 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
coenzyme Q8A/Chaperone activity of bc1 complex-like, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60]
ChEMBL Inhibition of ADCK3 B 6 pKd >1000 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
GtoPdb In a biochemical assay. - 6.72 pKd 190 nM Kd J Med Chem (2011) 54: 2255-65 [PMID:21375264]
ChEMBL Binding affinity to JNK1 B 6.72 pKd 190 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of JNK1 B 6.72 pKd 190 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
ChEMBL Inhibition of JNK1 (unknown origin) B 5.27 pIC50 5420 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 424-428 [PMID:26704265]
mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
ChEMBL Binding affinity to JNK2 B 7.8 pKd 16 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of JNK2 B 7.8 pKd 16 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
GtoPdb In a biochemical assay. - 7.8 pKd 16 nM Kd J Med Chem (2011) 54: 2255-65 [PMID:21375264]
mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
GtoPdb In a biochemical assay. - 7.72 pKd 19 nM Kd J Med Chem (2011) 54: 2255-65 [PMID:21375264]
ChEMBL Binding affinity to JNK3 B 7.72 pKd 19 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of JNK3 B 7.72 pKd 19 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
ChEMBL Inhibition of DDR1 B 6 pKd >1000 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Binding affinity to p38alpha B 8.89 pKd 1.3 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of p38alpha B 8.89 pKd 1.3 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
GtoPdb In a biochemical assay. - 8.89 pKd 1.3 nM Kd J Med Chem (2011) 54: 2255-65 [PMID:21375264]
ChEMBL Inhibition of human recombinant p38alpha by liquid scintillation counting B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of human recombinant p38alpha assessed as incorporation of 33P from gamma-[33P]ATP into myelin basic protein after 30 mins by scintillation counting B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
GtoPdb In a biochemical assay. - 6.92 pKd 120 nM Kd J Med Chem (2011) 54: 2255-65 [PMID:21375264]
ChEMBL Binding affinity to p38beta B 6.92 pKd 120 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of P38beta B 6.92 pKd 120 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Inhibition of RSK2 B 6.52 pKd 300 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
ChEMBL Inhibition of RSK4 B 6.82 pKd 150 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
serine/threonine kinase 36/Serine/threonine-protein kinase 36 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4312] [GtoPdb: 2223] [UniProtKB: Q9NRP7]
ChEMBL Inhibition of STK36 B 6 pKd >1000 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
cyclin G associated kinase/Serine/threonine-protein kinase GAK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976]
ChEMBL Inhibition of GAK B 6 pKd >1000 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]
nemo like kinase/Serine/threonine protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8]
ChEMBL Binding affinity to NLK B 6.77 pKd 170 nM Kd J. Med. Chem. (2010) 53: 2345-2353 [PMID:19950901]
ChEMBL Inhibition of NLK B 6.77 pKd 170 nM Kd J. Med. Chem. (2011) 54: 2255-2265 [PMID:21375264]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]