RS-17053 [Ligand Id: 495] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL88272 (RS-17053) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 affinity was tested on human Alpha-1A adrenergic receptor | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; FEBS Lett (1998) 422: 279-83 [PMID:9490024]; Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]; Mol Pharmacol (1996) 49: 209-15 [PMID:8632751]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824] | ||||||||
| ChEMBL | Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay | F | 7.3 | pKd | 50.12 | nM | Kd | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| 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 | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
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]
