RS-100329 [Ligand Id: 7381] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL56331 (RS-100329) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor | B | 9.6 | pKi | 0.25 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1873-1878 [PMID:12749888] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - |
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active | B | 9.6 | pKi | 0.25 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832] |
| ChEMBL | Antagonist inhibition of noradrenaline-stimulated contractions of rabbit bladderneck (RBN) for Alpha-1A adrenergic receptor | F | 9.2 | pA2 | 9.2 | - | 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] | ||||||||
| ChEMBL | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1B adrenergic receptor | B | 7.5 | pKi | 31.62 | 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 | Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1D adrenergic receptor | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1873-1878 [PMID:12749888] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 | 7.9 | pA2 | 7.9 | - | pA2/pKB | Bioorg Med Chem Lett (2003) 13: 1873-1878 [PMID:12749888] |
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]
