(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 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]
