zacopride [Ligand Id: 245] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18041 (Zacopride) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941] | ||||||||
| ChEMBL | Antagonist activity at rat alpha-7 nicotinic acetylcholine receptor expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced currents preincubated for 10 mins followed by nicotine induction by two-electrode voltage-clamp electrophysiology assay | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3184-3188 [PMID:26087938] |
| ChEMBL | Antagonist activity at rat alpha-7 nicotinic acetylcholine receptor expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced currents preincubated for 10 mins followed by nicotine induction by two-electrode voltage-clamp electrophysiology assay | B | 5.15 | pIC50 | 7040 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3184-3188 [PMID:26087938] |
| 5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| ChEMBL | Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated guinea pig ileum (GPI) | F | 8.5 | pKd | 3.16 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN) | F | 10.1 | pKd | 0.08 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | In vitro antagonism of the 5-HT-3 receptor determined by inhibition of 5-HT-induced depolarization of the isolated rat vagus nerve. | F | 9.1 | pKd | 0.79 | nM | Kd | J Med Chem (1992) 35: 1515-1520 [PMID:1578478] |
| ChEMBL | Displacement of the 5-hydroxytryptamine 3 receptor ligand [3H]GR-65630 from rat brain cortical membranes. | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (1992) 35: 895-903 [PMID:1312602] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 in rat posterior cortex | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand | B | 9.38 | pKi | 0.42 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | In vitro displacement of [3H]-LY 278584 from rat cerebral cortex 5-hydroxytryptamine 3 receptor | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 1195-1198 |
| ChEMBL | pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor | B | 9.38 | pKi | 0.42 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | Binding affinity was evaluated in vitro by displacement of [3H]zacopride radioligand from 5-hydroxytryptamine 3 receptor | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 245-248 |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | In vitro binding affinity for the 5-hydroxytryptamine 3 receptor was determined with NG-108-15 mouse neuroblastoma-glioma cells | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1990) 33: 2721-2725 [PMID:2145434] |
| ChEMBL | Displacement of [3H]GR65630 from 5-HT3 receptor (unknown origin) | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| ChEMBL | Displacement of [3H]GR65630 from 5-HT3 receptor (unknown origin) | B | 9.41 | pKi | 0.39 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563] | ||||||||
| ChEMBL | Compound was tested for its antagonistic activity against 5-hydroxytryptamine 3 receptor in rat brain using [3H]zacopride as the radioligand. | F | 9.22 | pKd | 0.6 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 2657-2662 |
| 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - |
EMBO J (1995) 14: 2806-15 [PMID:7796807]; J Neurochem (1998) 70: 2252-61 [PMID:9603189]; Neuroreport (1997) 8: 3189-96 [PMID:9351641] |
| 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | - | - | - | FEBS Lett (1996) 398: 19-25 [PMID:8946946] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum | B | 6.12 | pKi | 753 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
| ChEMBL | Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor | B | 6.8 | pKi | 158 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 1195-1198 |
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606]; Neuropharmacology (1997) 36: 671-9 [PMID:9225293] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum | F | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 4.8 | pKi | 16000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
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]
