JAK3 inhibitor IV [Ligand Id: 5994] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL596674
  • Protein-glutamine gamma-glutamyltransferase in Guinea pig [ChEMBL: CHEMBL3308976] [UniProtKB: Q7M0F8]
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  • Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
  • CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 [ChEMBL: CHEMBL4523582] [GtoPdb: 3125313932063261] [UniProtKB: P0DTD1]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • Janus kinase 1 in Human [GtoPdb: 2047] [UniProtKB: P23458]
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  • transglutaminase 2 in Human [GtoPdb: 3015] [UniProtKB: P21980]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Protein-glutamine gamma-glutamyltransferase in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308976] [UniProtKB: Q7M0F8]
ChEMBL Inhibition of guinea pig liver transglutaminase B 5.4 pIC50 4000 nM IC50 Bioorg Med Chem Lett (2010) 20: 1141-1144 [PMID:20053561]
Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
ChEMBL MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate F 5.09 pIC50 8100 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125313932063261] [UniProtKB: P0DTD1]
ChEMBL SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate F 6.24 pIC50 580 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
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) by ELISA B 7.1 pIC50 80 nM IC50 Bioorg Med Chem Lett (2017) 27: 4229-4237 [PMID:28844493]
GtoPdb - - 7.1 pIC50 79 nM IC50 Bioorg Med Chem Lett (2000) 10: 575-9 [PMID:10741557]
Janus kinase 1 in Human [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb - - 4.4 pIC50 39810 nM IC50 Bioorg Med Chem Lett (2000) 10: 575-9 [PMID:10741557]
transglutaminase 2 in Human [GtoPdb: 3015] [UniProtKB: P21980]
GtoPdb In the absence of DTT. - 8 pIC50 10 nM IC50 Chem Biol (2008) 15: 969-78 [PMID:18804034]

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]