zacopride [Ligand Id: 245] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18041 (Zacoprida, 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 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]
