peficitinib [Ligand Id: 8315] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3137308 (Asp-015k, ASP-015K, ASP015K, JNJ-54781532, Peficitinib)
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Pharmacol Sci (2017) 133: 25-33 [PMID:28117214]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.41 pIC50 3.9 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.41 pIC50 3.9 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of human JAK1 using Biotin-Lyn-Substrate-2 as substrate assessed as reduction in rate of substrate phosphorylation incubated for 1 hr in presence of ATP by ELISA method B 8.41 pIC50 3.9 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Pharmacol Sci (2017) 133: 25-33 [PMID:28117214]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of human JAK2 using Biotin-Lyn-Substrate-2 as substrate assessed as reduction in rate of substrate phosphorylation incubated for 1 hr in presence of ATP by ELISA method B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) B 9.15 pIC50 0.71 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK3 (unknown origin) B 9.15 pIC50 0.7 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of human JAK3 using Biotin-Lyn-Substrate-2 as substrate assessed as reduction in rate of substrate phosphorylation incubated for 1 hr in presence of ATP by ELISA method B 9.15 pIC50 0.7 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Pharmacol Sci (2017) 133: 25-33 [PMID:28117214]
ChEMBL Inhibition of Tyk2 (unknown origin) B 8.32 pIC50 4.8 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of TYK2 (unknown origin) B 8.32 pIC50 4.8 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of human TYK2 using Biotin-IRS1-Substrate as substrate assessed as reduction in rate of substrate phosphorylation incubated for 1 hr in presence of ATP by ELISA method B 8.32 pIC50 4.8 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]

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]