tropisetron [Ligand Id: 260] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL56564 (ICS-205-930, Navoban, Novaban, NSC-759842, SDZ-ICS-930, Tropisetron, Tropisetron (as hydrochloride), Tropisetron hcl, Tropisetron hydrochloride, Tropisetron monohydrochloride) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907588] [GtoPdb: 462, 475, 471, 476] [UniProtKB: P02708, P07510, P11230, Q07001] | ||||||||
| ChEMBL | In vitro Binding affinity towards alpha-1-beta-1-gamma-delta nAChR was determined | B | 4.57 | pKi | 27000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D2 in rat was evaluated | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 189-192 [PMID:11755351] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.61 | pKi | 2479 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.46 | pIC50 | 3450 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| ChEMBL | Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes | F | 5.74 | pIC50 | 1800 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1849-1853 [PMID:15050614] |
| nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| ChEMBL | In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined | B | 4.26 | pKi | 55000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Inhibition constant against nicotinic acetylcholine receptor alpha7 | B | 8.16 | pKi | 6.9 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Binding affinity to alpha7 nAChR | B | 8.16 | pKi | 6.9 | nM | Ki | J Med Chem (2011) 54: 7943-7961 [PMID:21919481] |
| ChEMBL | Effective concentration that causes inhibition of alpha-7 nAChR, was determined. Values are expressed as EC50 +/- SEM. | F | 5.89 | pEC50 | 1300 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| ChEMBL | Agonist activity at alpha7 nAChR | F | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (2011) 54: 7943-7961 [PMID:21919481] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3365] [GtoPdb: 468] [UniProtKB: P49582] | ||||||||
| ChEMBL | In vitro Binding affinity towards alpha-7 nAChR was determined | B | 8.16 | pKi | 6.9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| 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 | Partial agonist activity at rat alpha-7 nicotinic acetylcholine receptor expressed in Xenopus oocytes assessed as induction of currents | B | 5.89 | pEC50 | 1300 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 3184-3188 [PMID:26087938] |
| ChEMBL | Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes | B | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 1849-1853 [PMID:15050614] |
| nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor subunit alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3068] [GtoPdb: 464] [UniProtKB: P32297] | ||||||||
| ChEMBL | In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined | B | 4.8 | pKi | 16000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibition constant against 5-hydroxytryptamine 1A receptor | B | 8.28 | pKi | 5.3 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| 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 | Binding affinity to 5-hydroxytryptamine 3 receptor entirely in guinea pig ileum | B | 7.9 | pKd | 12.59 | nM | Kd | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor of isolated guinea pig ileum (GPI) | F | 7.9 | pKd | 12.59 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor of neuronal in the afferent rabbit vagus | B | 10.2 | pKd | 0.06 | nM | Kd | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN) | F | 10.2 | pKd | 0.06 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH) | F | 10.6 | pKd | 0.03 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Binding affinity of compound towards 5-hydroxytryptamine 3 receptor using [3H]-BRL-43694 (1 nM) ligand in NG cells 108-15 was determined | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| ChEMBL | In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determined | B | 8.28 | pKi | 5.3 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (1998) 41: 311-317 [PMID:9464362] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | In vitro displacement of [3H]ICS-205-930 from 5-hydroxytryptamine 3 receptor in cultured NG-108-15 rat glioma cells | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (1990) 33: 13-16 [PMID:2296012] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor in rat brain cortical membranes using radioligand [3H]quipazine | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1993) 36: 2645-2657 [PMID:8410977] |
| ChEMBL | Concentration that inhibits the binding of radioligand, [3H]-ICS 205930, to 5-hydroxytryptamine 3 receptor from rat cortex | B | 8.77 | pKi | 1.71 | nM | Ki | J Med Chem (1990) 33: 2101-2108 [PMID:1695682] |
| ChEMBL | In vitro by displacement of [3H]LY-278584 from 5-hydroxytryptamine 3 receptor on rat entorhinal cortex | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (1997) 40: 586-593 [PMID:9046349] |
| ChEMBL | In vitro affinity for 5-hydroxytryptamine 3 (5-HT3) receptor by displacement of [3H]BRL-43694 from rat entorhinal cortex | B | 8.8 | pKi | 1.57 | nM | Ki | J Med Chem (1997) 40: 3369-3380 [PMID:9341912] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 3 receptor was evaluated | B | 8.81 | pKi | 1.55 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 189-192 [PMID:11755351] |
| ChEMBL | pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor | B | 8.89 | pKi | 1.29 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| 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 | 8.89 | pKi | 1.28 | 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 | 8.89 | pKi | 1.28 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 1195-1198 |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 3 receptor | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 695-698 |
| ChEMBL | Binding affinity was evaluated in vitro by displacement of [3H]zacopride radioligand from 5-hydroxytryptamine 3 receptor | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 245-248 |
| ChEMBL | Inhibition of 5-HT (1 ug/mL) induced depolarization in rat vagus nerve (5-hydroxytryptamine 3 receptor antagonism) | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 695-698 |
| ChEMBL | Compound was evaluated for the displacement of [3H]Q-ICS-205-930 from 5-HT3 recognition sites in rat brain membranes | B | 8.9 | pIC50 | 1.26 | nM | IC50 | J Med Chem (1992) 35: 1019-1031 [PMID:1552497] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Inhibition of 5HT3 receptor | B | 8.28 | pKi | 5.3 | nM | Ki | J Med Chem (2011) 54: 7943-7961 [PMID:21919481] |
| ChEMBL | Binding affinity at 5HT3 receptor | B | 8.55 | pKi | 2.82 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 3 receptor by displacement of [3H]2 in Neuroblastoma-Glioma NG-108-15 cells | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (1990) 33: 2715-2720 [PMID:2213824] |
| ChEMBL | In vitro binding affinity for the 5-hydroxytryptamine 3 receptor was determined with NG-108-15 mouse neuroblastoma-glioma cells | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (1990) 33: 2721-2725 [PMID:2145434] |
| Serotonin 3a (5-HT3a) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3666] [UniProtKB: O70212] | ||||||||
| ChEMBL | Antagonist activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as inhibition of serotonin-induced maximum response by competitive binding assay | B | 7.52 | pKd | 30.2 | nM | Kd | J Med Chem (2009) 52: 3548-3562 [PMID:19425598] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Binding affinity at 5HT4 receptor | B | 6.7 | pKi | 199.53 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - |
J Neurochem (1997) 69: 1810-9 [PMID:9349523]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2183] [GtoPdb: 9] [UniProtKB: P97288] | ||||||||
| ChEMBL | Tested for ability to stimulate 5-hydroxytryptamine 4 receptors in mouse Coliculi neurons | B | 6.2 | pKi | 6.2 | nM | Log Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| GtoPdb | - | - | 7.1 | 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] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - | Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606] |
| ChEMBL | Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 1195-1198 |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum. | F | 5.7 | pKd | 1995.26 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated | B | 6.9 | pKi | 125.1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 189-192 [PMID:11755351] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) | B | 7.27 | pKi | 54 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP) | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) | B | 6.49 | pIC50 | 324 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 6.59 | pKi | 259 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 6.31 | pIC50 | 488 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT3A in Human [GtoPdb: 379] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | 1.5 | nM | Ki |
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620]; Mol Pharmacol (1998) 53: 202-12 [PMID:9463477] |
| glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415] | ||||||||
| GtoPdb | - | - | 4.1 | pKi | 84000 | nM | Ki | |
| glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | 13000 | nM | Ki | |
| glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | 5400 | nM | Ki | |
| Glycine Receptor (All subtypes) in Human [GtoPdb: 428] | ||||||||
| GtoPdb | - | - | 4.1 | pIC50 | - | - | - |
J Neurochem (1999) 73: 802-6 [PMID:10428078]; J Neurochem (2007) 100: 758-69 [PMID:17181559] |
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]
