benzamil [Ligand Id: 4145] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL212579 (Benzamil)
  • Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
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  • ENaC α/Amiloride-sensitive sodium channel alpha-subunit in Human [ChEMBL: CHEMBL1791] [GtoPdb: 738] [UniProtKB: P37088]
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  • TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
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  • ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
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  • ENaCαβγ in Human [GtoPdb: 742]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
ChEMBL Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis B 5.55 pIC50 2790 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
ENaC α/Amiloride-sensitive sodium channel alpha-subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1791] [GtoPdb: 738] [UniProtKB: P37088]
ChEMBL Inhibition of dog bronchi prototypical epithelial sodium channel by electrophysiological assay B 7.18 pIC50 66 nM IC50 J Med Chem (2006) 49: 4098-4115 [PMID:16821771]
TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
GtoPdb - - 6 pIC50 1100 nM IC50
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
GtoPdb - - 5 pIC50 10000 nM IC50 Nature (1997) 386: 173-7 [PMID:9062189]
ENaCαβγ in Human [GtoPdb: 742]
GtoPdb - - 8 pIC50 ~10 nM IC50

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]