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]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 BovinepKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1d adrenergic receptorpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D2 receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1a (5-HT1a) receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2a (5-HT2a) receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
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];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]