upidosin [Ligand Id: 496] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL278865 (Upidosin)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]