(R)-zacopride [Ligand Id: 2288] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL27846 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity was evaluated by 5-hydroxytryptamine 1A receptor agonism in the pig cortex by displacing 8-OH-DPAT | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity was evaluated by 5-hydroxytryptamine 2A receptor agonism in the rat cortex by displacing ketanserin | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
| 5-HT3A/5-hydroxytryptamine receptor 3A 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 | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
| 5-HT4 receptor/5-hydroxytryptamine receptor 4 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 | 5.82 | pKi | 1510 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae | F | 6.3 | pEC50 | 501.19 | nM | EC50 | Bioorg Med Chem Lett (1993) 3: 1375-1378 |
| 5-hydroxytryptamine receptor 4 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 | 5.55 | pKi | 2818.38 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
| 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 | 6.78 | pEC50 | 166 | nM | EC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| Alpha-1A adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding affinity was evaluated by Alpha-1 adrenergic receptor in calf cortex by displacing prazosin | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| D(1A) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Binding affinity was evaluated by Dopamine receptor D1 agonism in the calf striatum by displacing SCH 23390 | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
| D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| D(2) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Binding affinity was evaluated by Dopamine receptor D2 agonism in the calf striatum by displacing spiperone | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
| D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | The ability to inhibit [3H]domperidone binding to dopamine receptor D2 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of racemic [3H]zacopride from rat cortex | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor was determined in rat cerebro cortical membranes using [3H]quipazine. | B | 8.5 | pKi | 3.16 | 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 | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1993) 36: 2645-2657 [PMID:8410977] |
| ChEMBL | Binding affinity at 5-hydroxytryptamine 3 receptor in rat posterior cortex by [3H]-BRL 43694 displacement. | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 691-694 |
| ChEMBL | Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1555-1558 |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor in rat entorhinal cortex using [3H]-BRL 43694 as radioligand | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 945-948 |
| 5-HT3AB in Human [GtoPdb: 378] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
| 5-HT3A in Human [GtoPdb: 379] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
ChEMBL data shown on this page come from version 36:
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]
