AZ960 [Ligand Id: 8476] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1774055
  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 V617F mutant (unknown origin) using L-Ahx-IPTSPITTTYFFFKKK-COOH as substrate in presence of ATP B 9.35 pKi 0.45 nM Ki Bioorg Med Chem (2016) 24: 4647-4651 [PMID:27519462]
GtoPdb - - 9.35 pKi 0.45 nM Ki J Biol Chem (2008) 283: 32334-43 [PMID:18775810]
ChEMBL Inhibition of JAK2 after 60 min B 8.52 pIC50 <3 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 after 60 min B 8.05 pIC50 9 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]

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]