(R)-zacopride [Ligand Id: 2288] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL27846
  • 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 BovinepKi BovinepIC50 BovinepEC50 BovinepKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuDopamine D1 receptorpKd BovinepKi BovinepIC50 BovinepEC50 BovinepKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuDopamine D2 receptorpKd BovinepKi BovinepIC50 BovinepEC50 BovinepKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1a (5-HT1a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.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 Rat0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3 (5-HT3) receptorpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3a (5-HT3a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 4 (5-HT4) receptorpKd RatpKi RatpIC50 RatpEC50 RatpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig02468Highcharts.com
  • 5-HT3AB in Human [GtoPdb: 378]
Created with Highcharts 10.3.3ValuesChart context menu5-HT3ABpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 5-HT3A in Human [GtoPdb: 379]
Created with Highcharts 10.3.3ValuesChart context menu5-HT3ApKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity was evaluated by Alpha-1 adrenergic receptor in calf cortex by displacing prazosin B 5 pKd <5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain B 5 pKi >10000 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity was evaluated by Dopamine receptor D1 agonism in the calf striatum by displacing SCH 23390 B 5 pKd <5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata B 5 pKi >10000 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity was evaluated by Dopamine receptor D2 agonism in the calf striatum by displacing spiperone B 5 pKd <5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL The ability to inhibit [3H]domperidone binding to dopamine receptor D2 in rat striata B 5 pKi >10000 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 1A receptor agonism in the pig cortex by displacing 8-OH-DPAT B 5 pKd <5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 2A receptor agonism in the rat cortex by displacing ketanserin B 5 pKd <5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor B 8.1 pKi 8 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of racemic [3H]zacopride from rat cortex B 8.43 pKi 3.71 nM Ki Bioorg Med Chem Lett (1996) 6: 477-480
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor was determined in rat cerebro cortical membranes using [3H]quipazine. B 8.5 pKi 3.16 nM Ki Bioorg Med Chem Lett (1993) 3: 1375-1378
ChEMBL Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor in rat brain cortical membranes using radioligand [3H]quipazine B 8.5 pKi 3.16 nM Ki J Med Chem (1993) 36: 2645-2657 [PMID:8410977]
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat posterior cortex by [3H]-BRL 43694 displacement. B 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (1992) 2: 691-694
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. B 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (1993) 3: 1555-1558
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor in rat entorhinal cortex using [3H]-BRL 43694 as radioligand B 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (1994) 4: 945-948
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of [3H](R)-zacopride from ondansetron-treated NG-108-15 cell membranes B 8.3 pKi 5.01 nM Ki Bioorg Med Chem Lett (1996) 6: 477-480
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand B 5.82 pKi 1510 nM Ki J Med Chem (1997) 40: 608-621 [PMID:9046352]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae F 6.3 pEC50 501.19 nM EC50 Bioorg Med Chem Lett (1993) 3: 1375-1378
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum. B 5.55 pKi 2818.38 nM Ki Bioorg Med Chem Lett (1996) 6: 477-480
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum F 6.78 pEC50 166 nM EC50 J Med Chem (1997) 40: 608-621 [PMID:9046352]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 7.7 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 7.9 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]

ChEMBL data shown on this page come from version 35:

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]