A61603 [Ligand Id: 480] 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: 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]
  • 7.92
1 CHEMBL109783_lig_chart_1 Alpha-1a adrenergic receptor HumanBovineRat
There should be some charts here, you may need to enable JavaScript!
  • Alpha-1b adrenergic receptor in Hamster [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
  • 0
2 CHEMBL109783_lig_chart_2 Alpha-1b adrenergic receptor HamsterRat
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
  • 5.83
3 CHEMBL109783_lig_chart_3 Alpha-1d adrenergic receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • This target only has 1 pki data point
  • 7.48
4 CHEMBL109783_lig_chart_4 Alpha-2a adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
  • This target only has 1 pki data point
  • 6.61
5 CHEMBL109783_lig_chart_5 Alpha-2b adrenergic receptor Rat
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]
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 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]