cofrogliptin [Ligand Id: 13765] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4646510 (Cofrogliptin, Cofrogliptina, Cofrogliptine, Haisco hsk 7653)
  • dipeptidyl peptidase 4/Dipeptidyl peptidase 4 in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
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  • dipeptidyl peptidase 8/Dipeptidyl peptidase 8 in Human [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
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  • dipeptidyl peptidase 9/Dipeptidyl peptidase 9 in Human [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
dipeptidyl peptidase 4/Dipeptidyl peptidase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
ChEMBL Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate B 8.38 pIC50 4.2 nM IC50 J Med Chem (2020) 63: 7108-7126 [PMID:32452679]
ChEMBL Inhibition of DPP4 (unknown origin) B 8.38 pIC50 4.18 nM IC50 Eur J Med Chem (2024) 272: 116464-116464 [PMID:38704940]
GtoPdb - - 8.38 pIC50 4.2 nM IC50 J Med Chem (2020) 63: 7108-7126 [PMID:32452679]
dipeptidyl peptidase 8/Dipeptidyl peptidase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
ChEMBL Inhibition of human recombinant DPP8 incubated for 15 mins using Gly-Pro-7-AMC substrate B 4 pIC50 >100000 nM IC50 J Med Chem (2020) 63: 7108-7126 [PMID:32452679]
dipeptidyl peptidase 9/Dipeptidyl peptidase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
ChEMBL Inhibition of human recombinant DPP9 incubated for 15 mins using Gly-Pro-7-AMC substrate B 4 pIC50 >100000 nM IC50 J Med Chem (2020) 63: 7108-7126 [PMID:32452679]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by manual whole-cell patch-clamp assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2020) 63: 7108-7126 [PMID:32452679]

ChEMBL data shown on this page come from version 36:

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]