(S)-zacopride [Ligand Id: 2289] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL28992 |
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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: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| 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 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]
