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ChEMBL ligand: CHEMBL24777 (Ro-700004, RS-100975) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832] |
ChEMBL | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor | B | 8.9 | pKi | 1.26 | nM | Ki | Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888] |
GtoPdb | - | - | 8.9 | pKi | - | - | - | Br J Pharmacol (1999) 127: 252-8 [PMID:10369480] |
ChEMBL | Binding affinity was tested on human Alpha-1A adrenergic receptor | B | 9 | pKi | 1 | nM | Ki | J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028] |
ChEMBL | Antagonist inhibition of noradrenaline-stimulated contractions of rabbit bladderneck (RBN) for Alpha-1A adrenergic receptor | F | 8.9 | pA2 | 8.9 | - | pA2/pKB | Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
GtoPdb | - | - | 7.1 | pKi | - | - | - | Br J Pharmacol (1999) 127: 252-8 [PMID:10369480] |
ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 7.1 | pKi | 79.43 | nM | Ki | J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028] |
ChEMBL | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1B adrenergic receptor | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 7 | pKi | 100 | nM | Ki | J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028] |
ChEMBL | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1D adrenergic receptor | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888] |
GtoPdb | - | - | 7.2 | pKi | - | - | - | Br J Pharmacol (1999) 127: 252-8 [PMID:10369480] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
ChEMBL | Antagonist inhibition noradrenaline-stimulated contractions of rat aortic strings for Alpha-1D adrenergic receptor | F | 6.8 | pA2 | 6.8 | - | pA2/pKB | Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888] |
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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]