PF-956980 [Ligand Id: 11060] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4068357
  • 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]
ChEMBL Inhibition of GST tagged human recombinant JAK1 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay B 7.43 pIC50 37.5 nM IC50 J Med Chem (2017) 60: 767-786 [PMID:27983835]
GtoPdb - - 8.12 pIC50 7.5 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
ChEMBL Inhibition of human JAK1 using 5FAM-KKSRGDYMTMQID as substrate by caliper microfluidic mobility shift assay B 8.12 pIC50 7.5 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay B 6.91 pIC50 123.6 nM IC50 J Med Chem (2017) 60: 767-786 [PMID:27983835]
ChEMBL Inhibition of human JAK2 using FITC-KGGEEEEYFELVKK as substrate by caliper microfluidic mobility shift assay B 8.15 pIC50 7.1 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
GtoPdb - - 8.15 pIC50 7.1 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of GST tagged human recombinant JAK3 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay B 6.86 pIC50 139.3 nM IC50 J Med Chem (2017) 60: 767-786 [PMID:27983835]
GtoPdb - - 8.55 pIC50 2.8 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
ChEMBL Inhibition of human JAK3 using FITC-KGGEEEEYFELVKK as substrate by caliper microfluidic mobility shift assay B 8.55 pIC50 2.8 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of Tyk2 (unknown origin) using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay B 5.79 pIC50 1632.2 nM IC50 J Med Chem (2017) 60: 767-786 [PMID:27983835]
GtoPdb - - 6.89 pIC50 128 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
ChEMBL Inhibition of human TYK2 using 5FAM-KKSRGDYMTMQID as substrate by caliper microfluidic mobility shift assay B 6.89 pIC50 128 nM IC50 J Med Chem (2020) 63: 11330-11361 [PMID:32352776]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]