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 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]
