(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]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 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]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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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: 373374] [UniProtKB: P35563Q9JJ16]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]