alfuzosin [Ligand Id: 7109] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL709 (Alfuzosin, NSC-760065, Uroxatral)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of AChE (unknown origin) B 7.74 pIC50 18 nM IC50 Bioorg Med Chem (2018) 26: 1511-1522 [PMID:29429576]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL In vitro antagonistic activity against alpha-1A receptor in dog prostate. F 6.66 pKd 218.78 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 8 pKi 10 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from human clone B 8.09 pKi 8.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 8.1 pKi 8.2 nM Ki Pharm Acta Helv (2000) 74: 163-71 [PMID:10812954]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from bovine clone B 7.64 pKi 23 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens F 7.61 pKd 24.55 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 7.92 pKi 12 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 8 pKi 10 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 8.55 pKi 2.8 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 8.6 pKi 2.8 nM Ki J Med Chem (1995) 38: 3415-44 [PMID:7658428]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL In vitro antagonistic activity against alpha-1B receptor in rat spleen. F 8.31 pKd 4.9 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 8.4 pKi 3.6 nM Ki Pharm Acta Helv (2000) 74: 163-71 [PMID:10812954]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.44 pKi 3.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8.5 pKi 3.16 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from rat clones. B 8.46 pKi 3.5 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 4.7 pIC50 19952.62 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform F 4.9 pIC50 12589.25 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay B 4.83 pIC50 14870 nM IC50 J Med Chem (2017) 60: 2685-2696 [PMID:28230985]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]