A-123189 [Ligand Id: 491] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13856 (A-123189)
  • 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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  • 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]
  • 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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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
ChEMBL Binding affinity for human Alpha-1A adrenergic receptor B 8.38 pKi 4.17 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 8.4 pKi - - - Bioorg. Med. Chem. Lett. (2001) 11: 1119-21 [PMID:11354357]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards bovine Alpha-1A adrenergic receptor B 9.46 pKi 0.35 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens B 8.36 pKd 4.37 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Binding affinity towards rat Alpha-1A adrenergic receptor B 8.46 pKi 3.47 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 8.5 pKi - - - Bioorg. Med. Chem. Lett. (2001) 11: 1119-21 [PMID:11354357]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 8 pKi - - - Bioorg. Med. Chem. Lett. (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards human Alpha-1B adrenergic receptor B 8.04 pKi 9.09 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL In vitro functional activity at Alpha-1B adrenergic receptor in rat spleen F 8.76 pKd 1.74 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 9.5 pKi - - - Bioorg. Med. Chem. Lett. (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards human Alpha-1D adrenergic receptor B 9.51 pKi 0.31 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL In vitro functional activity at Alpha-1D receptor in rat aorta B 10.7 pKd 0.02 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Binding affinity towards rat Alpha-1D adrenergic receptor B 9.77 pKi 0.17 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 9.8 pKi - - - Bioorg. Med. Chem. Lett. (2001) 11: 1119-21 [PMID:11354357]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptor B 7.08 pKi 82.5 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Ancillary Binding affinity towards rat alpha-2B receptor B 7.18 pKi 66.6 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Ancillary Binding affinity to cloned human Alpha-2C adrenergic receptor B 7.09 pKi 82 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Ancillary Binding affinity to rat Dopamine receptor D1 B 4.91 pKi 12300 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Ancillary Binding affinity towards rat Dopamine receptor D2 B 7.77 pKi 17 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1119-1121 [PMID:11354357]

ChEMBL data shown on this page come from version 27:

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]