compound 12 [PMID: 26238322] [Ligand Id: 13151] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3609360
  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2015) 25: 3921-3923 [PMID:26238322]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 9.8 pKi - - - Bioorg Med Chem Lett (2015) 25: 3921-3 [PMID:26238322]
ChEMBL Antagonist activity at human alpha1B adrenoceptor assessed as inhibition of norepinephrine-induced increase of intracellular calcium level by cell based assay F 6.25 pIC50 560 nM IC50 Bioorg Med Chem Lett (2015) 25: 3921-3923 [PMID:26238322]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Displacement of [3H]prazosin from alpha1B adrenoceptor in rat liver membranes B 9.21 pKi 0.61 nM Ki Bioorg Med Chem Lett (2015) 25: 3921-3923 [PMID:26238322]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity to human recombinant alpha1D adrenoceptor B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2015) 25: 3921-3923 [PMID:26238322]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]