A61603 [Ligand Id: 480] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL109783
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • Alpha-1b adrenergic receptor in Hamster [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
  • 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 Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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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]
GtoPdb - - 8.4 pIC50 - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
J Pharmacol Exp Ther (1995) 274: 97-103 [PMID:7616455]
ChEMBL In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate F 7.66 pEC50 21.88 nM EC50 J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor B 8.03 pEC50 9.3 nM EC50 J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards bovine clonal Alpha-1A adrenergic receptor B 7.52 pKi 30.2 nM Ki J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay B 7.92 pKi 12.02 nM Ki J. Med. Chem. (2004) 47: 3220-3235 [PMID:15163201]
ChEMBL Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015) B 7.92 pKi 12 nM Ki J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands B 8.05 pKi 8.91 nM Ki J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens F 8.24 pEC50 5.75 nM EC50 J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
ChEMBL In vitro binding affinity towards alpha-1B adrenergic receptor of hamster clone in radioligand binding assay B 5.53 pKi 2951.21 nM Ki J. Med. Chem. (2004) 47: 3220-3235 [PMID:15163201]
ChEMBL Binding affinity towards hamster cloned Alpha-1B adrenergic receptor; value ranges from (2.0 -4.4) B 5.54 pKi 2900 nM Ki J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
ChEMBL Binding affinity towards hamster clonal Alpha-1B adrenergic receptor B 5.68 pKi 2089.3 nM Ki J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Effective concentration in vitro against rat spleen Alpha-1B adrenergic receptor indicates EC50 < 15% at a concentration of 10 uM B 6.49 pEC50 320 nM EC50 J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
ChEMBL In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen F 6.5 pEC50 316.23 nM EC50 J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity towards rat cloned Alpha-1D adrenergic receptor; value ranges from (1.3 -1.6) B 5.82 pKi 1500 nM Ki J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
ChEMBL In vitro binding affinity towards alpha-1D adrenergic receptor of rat clone in radioligand binding assay B 5.83 pKi 1479.11 nM Ki J. Med. Chem. (2004) 47: 3220-3235 [PMID:15163201]
ChEMBL Binding affinity towards rat clonal Alpha-1D adrenergic receptor B 5.87 pKi 1348.96 nM Ki J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
ChEMBL Effective concentration in vitro against rat aorta Alpha-1D adrenergic receptor;* indicates EC50 < 15% at a concentration of 10 uM B 5.59 pEC50 2600 nM EC50 J. Med. Chem. (2002) 45: 4395-4397 [PMID:12238918]
ChEMBL In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta F 5.59 pEC50 2570.4 nM EC50 J. Med. Chem. (1996) 39: 4116-4119 [PMID:8831777]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay B 7.48 pKi 33.11 nM Ki J. Med. Chem. (2004) 47: 3220-3235 [PMID:15163201]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL In vitro binding affinity towards alpha-2B adrenergic receptor of rat neonatal lung in radioligand binding assay B 6.61 pKi 245.47 nM Ki J. Med. Chem. (2004) 47: 3220-3235 [PMID:15163201]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]