A-119637 [Ligand Id: 490] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL268758 (A-119637)
  • 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 Rat024681012Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1d adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat024681012Highcharts.com
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2b adrenergic receptorpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2c adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D1 receptorpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.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 Rat02468Highcharts.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 Binding affinity for human Alpha-1A adrenergic receptor B 8.58 pKi 2.63 nM Ki Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active B 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832]
GtoPdb - - 8.6 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 9.56 pKi 0.27 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 8.07 pKd 8.51 nM Kd Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 8.6 pKi - - - Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards rat Alpha-1A adrenergic receptor B 8.61 pKi 2.43 nM Ki Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 8.3 pKi - - - Bioorg Med Chem Lett (2001) 11: 1119-21 [PMID:11354357]
ChEMBL Binding affinity towards human Alpha-1B adrenergic receptor B 8.33 pKi 4.66 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 8.69 pKd 2.04 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]
ChEMBL Binding affinity towards human Alpha-1D adrenergic receptor B 9.6 pKi 0.25 nM Ki Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 9.6 pKi - - - Bioorg Med Chem Lett (2001) 11: 1119-21 [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 adrenergic receptor in rat aorta B 10.6 pKd 0.03 nM Kd Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
ChEMBL Binding affinity towards rat Alpha-1D adrenergic receptor B 9.67 pKi 0.21 nM Ki Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]
GtoPdb - - 9.7 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 7.11 pKi 77.8 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 7.15 pKi 71 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 7.13 pKi 74.7 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 5.22 pKi 6090 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 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (2001) 11: 1119-1121 [PMID:11354357]

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]