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 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]
