Ro-70-0004 [Ligand Id: 497] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
