SEN177 [Ligand Id: 13399] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4462495 |
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| 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] |
| ChEMBL | Inhibition of human glutaminyl cyclase assessed as inhibition constant | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2024) 97: 117542-117542 [PMID:38104495] |
| 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]
