upidosin [Ligand Id: 496] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278865 (Upidosin, Upidosina, Upidosine) |
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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 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]
