silodosin [Ligand Id: 493] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL24778 (Silodosin, Rapaflo, KAD-3213, KMD-3213)
  • 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]
  • 0
1 CHEMBL24778_lig_chart_1 Alpha-1a adrenergic receptor HumanRat
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • 7.7
2 CHEMBL24778_lig_chart_2 Alpha-1b adrenergic receptor Human
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • 8.7
3 CHEMBL24778_lig_chart_3 Alpha-1d adrenergic receptor Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
4 CHEMBL24778_lig_chart_4 HERG Human
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
  • This target only has 0 pki data point
  • 0
5 CHEMBL24778_lig_chart_5 Sodium channel protein type V alpha subunit Human
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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 - - 10.4 pKi - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 10.4 pKi 0.04 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active B 10.44 pKi 0.04 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
ChEMBL Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2016) 59: 3826-3839 [PMID:27031406]
ChEMBL Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay B 8.74 pIC50 1.8 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins B 9.1 pIC50 0.8 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 7.7 pKi - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.7 pKi 19.95 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Antagonist activity at human alpha-1B adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins B 6.27 pIC50 541.4 nM IC50 J. Med. Chem. (2016) 59: 3826-3839 [PMID:27031406]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 8.7 pKi - - - Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Antagonist activity at alpha-1D adrenergic receptor (unknown origin) transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins B 7.56 pIC50 27.3 nM IC50 J. Med. Chem. (2016) 59: 3826-3839 [PMID:27031406]
ChEMBL Antagonist activity at human full-length N-terminal SNAP-tagged alpha1D adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay B 8.2 pIC50 6.3 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 4.6 pIC50 25118.86 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of human ERG B 5.09 pIC50 8200 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 5.1 pIC50 7943.28 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 4.2 pIC50 63095.73 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

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]