(S)-zacopride [Ligand Id: 2289] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL28992
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
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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
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity against Dopamine receptor D2 using [3H]spiperone as radioligand in rat striatum B 6 pKi >1000 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Affinity of compound towards d Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand B 6 pKi >1000 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor was determined in rat cerebro cortical membranes using [3H]quipazine. B 9.6 pKi 0.25 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 9.6 pKi 0.25 nM Ki J. Med. Chem. (1993) 36: 2645-2657 [PMID:8410977]
ChEMBL Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 as radioligand in rat posterior cortex B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 1555-1558
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat posterior cortex by [3H]-BRL 43694 displacement. B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (1992) 2: 691-694
ChEMBL Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor in rat entorhinal cortex using [3H]-BRL 43694 as radioligand B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 945-948
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. B 9.96 pKi 0.11 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 263-266
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 5.3 pKi 5011.87 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 477-480
ChEMBL Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of [3H]-BRL 43694 from NG-108-15 cell membranes B 9.74 pKi 0.18 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 477-480
5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
ChEMBL Compound was evaluated in vivo for the antagonistic activity towards 5-hydroxytryptamine 3 receptor F 9.64 pKi 0.23 nM Ki Bioorg. Med. Chem. Lett. (1992) 2: 1613-1618
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 6.42 pKi 383 nM Ki J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]
ChEMBL Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum B 6.42 pKi 383 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement. B 6.88 pKi 131 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 263-266
ChEMBL Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay F 6.69 pEC50 203 nM EC50 Bioorg. Med. Chem. Lett. (1992) 2: 1613-1618
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (1993) 3: 1375-1378
ChEMBL In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. F 7.25 pEC50 55.9 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 263-266
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 6.36 pKi 436.52 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 477-480
ChEMBL Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor B 6.42 pKi 383 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
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 7.11 pEC50 77 nM EC50 J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 8.8 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 9 pKi 1 nM Ki Neuropharmacology (2001) 41: 282-4 [PMID:11489465]

ChEMBL data shown on this page come from version 28:

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]