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 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]