SEN177 [Ligand Id: 13399] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL4462495
  • glutaminyl-peptide cyclotransferase/Glutaminyl-peptide cyclotransferase in Human [ChEMBL: CHEMBL4508] [GtoPdb: 2411] [UniProtKB: Q16769]
There should be some charts here, you may need to enable JavaScript!
  • glutaminyl-peptide cyclotransferase like in Human [GtoPdb: 3289] [UniProtKB: Q9NXS2]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
glutaminyl-peptide cyclotransferase/Glutaminyl-peptide cyclotransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4508] [GtoPdb: 2411] [UniProtKB: Q16769]
ChEMBL Binding affinity to human QC assessed as inhibition constant B 7.7 pKi 20 nM Ki J Med Chem (2021) 64: 6549-6565 [PMID:34000808]
GtoPdb - - 7.7 pKi 20 nM Ki J Med Chem (2021) 64: 6549-6565 [PMID:34000808]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect cells using H-Gln-AMC hydrobromide as substrate measured in presence of pGAPase by fluorometric assay B 7.78 pIC50 16.7 nM IC50 J Med Chem (2019) 62: 8011-8027 [PMID:31411468]
ChEMBL Inhibition of human recombinant glutaminyl cyclase using H-Gln-AMC hydrobromide as substrate measured after 15 mins by fluorimetry B 7.78 pIC50 16.7 nM IC50 Eur J Med Chem (2021) 226: 113819-113819 [PMID:34536669]
GtoPdb - - 7.78 pIC50 16.7 nM IC50 J Med Chem (2019) 62: 8011-8027 [PMID:31411468]
glutaminyl-peptide cyclotransferase like in Human [GtoPdb: 3289] [UniProtKB: Q9NXS2]
GtoPdb - - 6.49 pIC50 321.1 nM IC50 Signal Transduct Target Ther (2023) 8: 454 [PMID:38097557]

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]