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

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ChEMBL ligand: CHEMBL1090089 (Pamapimod, R-1503, R1503, 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 34:

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]