upidosin [Ligand Id: 496] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278865 (Upidosin) |
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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 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 | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832] |
| ChEMBL | Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells) | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2003) 46: 3762-3765 [PMID:12904082] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - | Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens | F | 8.42 | pKd | 3.8 | nM | Kd | J Med Chem (2003) 46: 3762-3765 [PMID:12904082] |
| ChEMBL | Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| 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 | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248] |
| ChEMBL | Inhibition of [3H]-prazosin binding to cloned human Alpha-1B adrenergic receptor in CHO cells (chinese hamster ovary cells) | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2003) 46: 3762-3765 [PMID:12904082] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | Binding affinity was tested on CEC-pretreated rat liver Alpha-1B adrenergic receptor | B | 7.62 | pIC50 | 24 | nM | IC50 | 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] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248] |
| ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Inhibition of [3H]-prazosin binding to cloned human Alpha-1D adrenergic receptor in CHO cells (chinese hamster ovary cells) | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2003) 46: 3762-3765 [PMID:12904082] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor serotonergic receptor in human HeLa cells | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2003) 46: 3762-3765 [PMID:12904082] |
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]
