BMS-986202 [Ligand Id: 12723] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4789639 (Bms-986202, BMS986202)
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  • tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597]
  • tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Mouse [ChEMBL: CHEMBL2321619] [GtoPdb: 2269] [UniProtKB: Q9R117]
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  • 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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  • 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/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 20472049] [UniProtKB: P23458P52333]
ChEMBL Inhibition of JAK1/3 (unknown origin) by IL-2 dependent cell based assay B 4.9 pIC50 >12500 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597]
GtoPdb Binding affinity for Tyk2 JH2 domain - 10.7 pKi 0.02 nM Ki J Med Chem (2021) 64: 677-694 [PMID:33370104]
GtoPdb - - 9.72 pIC50 0.19 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321619] [GtoPdb: 2269] [UniProtKB: Q9R117]
ChEMBL Inhibition of TYK2 in mouse whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation B 6.32 pIC50 481 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 JH2 domain (unknown origin) B 8.11 pIC50 7.8 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) by EPO-stimulated cell based assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of TYK2 JH2 domain (unknown origin) by HTRF assay based Morrison titration analysis B 10.7 pKi 0.02 nM Ki J Med Chem (2021) 64: 677-694 [PMID:33370104]
GtoPdb Binding affinity for Tyk2 JH2 domain - 10.7 pKi 0.02 nM Ki J Med Chem (2021) 64: 677-694 [PMID:33370104]
ChEMBL Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation B 7.24 pIC50 58 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
ChEMBL Inhibition of TYK2 in IL-23 stimulated human Kit225 T cells by luciferase reporter gene assay B 7.92 pIC50 12 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
ChEMBL Inhibition of TYK2 in IFN-alpha stimulated human Kit225 T cells by luciferase reporter gene assay B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
GtoPdb - - 9.72 pIC50 0.19 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]
ChEMBL Inhibition of TYK2 JH2 domain (unknown origin) by HTRF assay B 9.72 pIC50 0.19 nM IC50 J Med Chem (2021) 64: 677-694 [PMID:33370104]

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]