alfuzosin [Ligand Id: 7109] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL709 (Alfuzosin, NSC-760065, Uroxatral) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (2019) 371: 106-112 [PMID:31285236] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 | - | - | - |
Pharm Acta Helv (2000) 74: 163-71 [PMID:10812954]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
