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 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]
