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ChEMBL ligand: CHEMBL1090089 (Pamapimod, R-1503, R1503, Ro-4402257, RO 4402257) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]