Ro-70-0004 [Ligand Id: 497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL24777 (Ro-700004, RS-100975)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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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 constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
ChEMBL Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor B 8.9 pKi 1.26 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888]
GtoPdb - - 8.9 pKi - - - Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
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 Antagonist inhibition of noradrenaline-stimulated contractions of rabbit bladderneck (RBN) for Alpha-1A adrenergic receptor F 8.9 pA2 8.9 - pA2/pKB Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 7.1 pKi - - - Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.1 pKi 79.43 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1B adrenergic receptor B 7.1 pKi 79.43 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 7 pKi 100 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1D adrenergic receptor B 7.2 pKi 63.1 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888]
GtoPdb - - 7.2 pKi - - - Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Antagonist inhibition noradrenaline-stimulated contractions of rat aortic strings for Alpha-1D adrenergic receptor F 6.8 pA2 6.8 - pA2/pKB Bioorg. Med. Chem. Lett. (2003) 13: 1873-1878 [PMID:12749888]

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]