Rec 15/2615 [Ligand Id: 8459] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL430717
  • 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]
1 CHEMBL430717_lig_chart_1 Alpha-1a adrenergic receptor HumanBovineRat
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
2 CHEMBL430717_lig_chart_2 Alpha-1b adrenergic receptor Human
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
  • This target only has 0 pki data point
3 CHEMBL430717_lig_chart_3 Alpha-1d adrenergic receptor Rat
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • This target only has 0 pki data point
4 CHEMBL430717_lig_chart_4 Dopamine D2 receptor Rat
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 0 pki data point
5 CHEMBL430717_lig_chart_5 Serotonin 1a (5-HT1a) receptor Rat
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
  • This target only has 0 pki data point
6 CHEMBL430717_lig_chart_6 Serotonin 2a (5-HT2a) receptor Rat
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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 The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line. B 7.99 pKi 10.34 nM Ki J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptor B 7.76 pIC50 17.2 nM IC50 J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line. B 8.12 pKi 7.5 nM Ki J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL The binding affinity towards Alpha-1B adrenergic receptor in the COS cell line. B 9.35 pKi 0.45 nM Ki J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]
GtoPdb - - 9.5 pKi - - - J. Pharmacol. Exp. Ther. (1997) 281: 1284-93 [PMID:9190864]
ChEMBL Binding affinity was tested on cloned hamster Alpha-1B adrenergic receptor B 8.92 pIC50 1.2 nM IC50 J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity was tested on cloned rat Alpha-1D adrenergic receptor B 7.64 pIC50 22.9 nM IC50 J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Inhibitory concentration against Dopamine receptor D2 (Inactive at >1000 nM concentration) B 6 pIC50 >1000 nM IC50 J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Inhibitory concentration against 5-hydroxytryptamine 1A receptor (Inactive at >1000 nM concentration) B 6 pIC50 >1000 nM IC50 J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Inhibitory concentration against 5-hydroxytryptamine 2A receptor (Inactive at >1000 nM concentration) B 6 pIC50 >1000 nM IC50 J. Med. Chem. (1999) 42: 427-437 [PMID:9986714]

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]