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ChEMBL ligand: CHEMBL4789639 (Bms-986202, BMS986202) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333] | ||||||||
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]