ondansetron [Ligand Id: 2290] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL46 (A04AA01, Desmethylondansetron, EUR-1025, GR-38032, GR-38032F, NSC-757870, Ondansetron, Zofran, Zofran odt, Zuplenz) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | The binding affinity was measured on alpha-2-adrenergic receptor using [3H]- clonidine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | The binding affinity was measured on cholecystokinin type A receptor using [3H]- CCK-8 as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| CCK2 receptor/Cholecystokinin B receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3508] [GtoPdb: 77] [UniProtKB: P30553] | ||||||||
| ChEMBL | The binding affinity was measured on cholecystokinin type B receptor using [3H]- CCK-8 as radioligand. | B | 6.17 | pKi | 680 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | The binding affinity was measured on delta-opiate receptor using [3H]- dadle as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | The binding affinity was measured on dopamine receptor D1 using [3H]- dopamine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | The binding affinity was measured on dopamine receptor D2 using [3H]- spiperone as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | Binding affinity against dopamine D2 receptor in rat brain synaptic membrane using [3H]-spiperone as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 619-624 [PMID:9871571] |
| ChEMBL | Inhibition of the binding of radioligand [3H]spiperone to dopamine receptor D2 in rat brain synaptic membrane | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 702-715 [PMID:12593651] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | The binding affinity was measured on dopamine receptor D3 using [3H]- dopamine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | Displacement of [3H]- Diazepam from rat GABA-A benzodiazepine receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | Displacement of [3H]DH-muscimol from rat GABA-A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | Non-competitive antagonist activity against Gamma-aminobutyric acid A (GABA-A) receptor | F | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2000) 43: 1427-1447 [PMID:10780899] |
| GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961] | ||||||||
| ChEMBL | The binding affinity was measured on NMDA receptor using [3H]- CGS-19755 as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| glycine receptor α4 subunit (pseudogene in humans)/Glycine receptor alpha-4 chain in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3500] [GtoPdb: 426] [UniProtKB: Q61603] | ||||||||
| ChEMBL | The binding affinity was measured on glycine receptor using [3H]- strychnine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 6.09 | pIC50 | 812.83 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 6.09 | pIC50 | 812.83 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 6.09 | pIC50 | 812.83 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibition of human ERG | B | 6.09 | pIC50 | 812.83 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibition of human ERG expressed in HEK cells by patch clamp technique | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6538-6541 [PMID:20889341] |
| H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
| ChEMBL | The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | The binding affinity was measured on histamine H3 receptor using [3H]- N-Me-histam as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| Interleukin-6 receptor, α subunit/Interleukin-6 receptor alpha chain in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4289] [GtoPdb: 1708] [UniProtKB: P22273] | ||||||||
| ChEMBL | The binding affinity was measured on leukotriene-6 receptor using [3H]- IL-6 as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | The binding affinity was measured on kappa-opiate receptor using [3H]- EKC as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| BLT1 receptor/Leukotriene B4 receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2126] [GtoPdb: 267] [UniProtKB: Q9R0Q2] | ||||||||
| ChEMBL | The binding affinity was measured on leukotriene-D4 receptor using [3H]- LTD4 as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | The binding affinity was measured on mu-opiate receptor using [3H]- naloxone as radioligand. | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | The binding affinity was measured on muscarine M1 receptor using [3H]- pirenzepine as radioligand. | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | The binding affinity was measured on muscarine M2 receptor using [3H]- N-Me-SCOPOL as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | The binding affinity was measured on muscarine M3 receptor using [3H]- N-Me-SCOPOL as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 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 | 4.57 | pIC50 | 27000 | 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 | 4.34 | pKi | 46000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| ChEMBL | Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes | F | 4.18 | pIC50 | 66000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1849-1853 [PMID:15050614] |
| 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 | 5.52 | pKi | >3000 | 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 | Inhibition of the response to ACh when coapplied with Nicotinic acetylcholine receptor alpha7 | B | 4.6 | pIC50 | 25000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1849-1853 [PMID:15050614] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | The binding affinity was measured on imidazoline I2 receptor using [3H]- indazoxan as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 1A receptor using [3H]- 8-OH-DPAT as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand. | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565] | ||||||||
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 1D receptor using [3H]- serotonin as radioligand. | B | 4.7 | pKi | 20000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells measured after 1.5 hrs by Microbeta plate reader method | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.34 | pKi | 456 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.14 | pIC50 | 717 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 1C receptor using [3H]- serotonin as radioligand. | B | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 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 against 5-hydroxytryptamine 3 receptor of guinea pig ileum | B | 7.01 | pKd | 97.72 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 667-672 |
| ChEMBL | Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor of isolated guinea pig ileum (GPI) | F | 7.1 | pKd | 79.43 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor entirely in guinea pig ileum | B | 7.3 | pKd | 50.12 | 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 | 9.2 | pKd | 0.63 | 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 | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart | B | 10.1 | pKd | 0.08 | nM | Kd | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH) | F | 10.1 | pKd | 0.08 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 461-466 |
| ChEMBL | In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determined | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 319-321 [PMID:11212100] |
| ChEMBL | Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (1993) 36: 3286-3292 [PMID:8230119] |
| 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 | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1992) 35: 1515-1520 [PMID:1578478] |
| ChEMBL | Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | In vitro displacement of [3H]ICS-205-930 from 5-hydroxytryptamine 3 receptor in cultured NG-108-15 rat glioma cells | B | 7.79 | pKi | 16.2 | nM | Ki | J Med Chem (1990) 33: 13-16 [PMID:2296012] |
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Binding affinity against radioligand [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in neuroblastoma-glioma (NG108-15) cells. | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (1993) 36: 617-626 [PMID:8496941] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]quipazine binding to 5-hydroxytryptamine 3 receptor sites in NG 108-15. | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (1992) 35: 4893-4902 [PMID:1479589] |
| ChEMBL | Displacement of binding of [3H]-BRL 43694 to 5-hydroxytryptamine 3 receptor in rat cerebral cortex | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (1993) 36: 2745-2750 [PMID:8410988] |
| ChEMBL | Displacement of the 5-hydroxytryptamine 3 receptor ligand [3H]GR-65630 from rat brain cortical membranes. | B | 8.21 | pKi | 6.16 | nM | Ki | J Med Chem (1992) 35: 895-903 [PMID:1312602] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex | B | 8.27 | pKi | 5.37 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex | B | 8.48 | pKi | 3.31 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (1998) 41: 311-317 [PMID:9464362] |
| 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 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 | 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 | 8.61 | pKi | 2.46 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor | B | 8.61 | pKi | 2.46 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 3 receptor from rat cortex using [3H]BRL-43694 as radioligand | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | In vitro affinity for 5-hydroxytryptamine 3 (5-HT3) receptor by displacement of [3H]BRL-43694 from rat entorhinal cortex | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1997) 40: 3369-3380 [PMID:9341912] |
| ChEMBL | Compound was evaluated for its in vitro affinity at serotonergic 5-hydroxytryptamine 3 receptor by radioligand binding assay, using [3H]-LY 278584 in rat cerebral cortex membranes. | B | 9.11 | pKi | 0.77 | nM | Ki | J Med Chem (1999) 42: 5020-5028 [PMID:10585211] |
| ChEMBL | Inhibition of [3H]BRL-43694 binding to rat 5-hydroxytryptamine 3 receptor | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (1994) 37: 1320-1325 [PMID:8176710] |
| ChEMBL | Binding affinity was evaluated in vitro by displacement of [3H]zacopride radioligand from 5-hydroxytryptamine 3 receptor | B | 8.15 | pIC50 | 7.1 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 245-248 |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor from rat cortical homogenate using [3H]zacopride as radioligand | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Compound was evaluated for the displacement of [3H]-Q-ICS 205-930 binding to 5-hydroxytryptamine 3 recognition sites in rat brain membranes | B | 8.71 | pIC50 | 1.95 | nM | IC50 | J Med Chem (1991) 34: 140-151 [PMID:1992112] |
| ChEMBL | Compound was evaluated for the displacement of [3H]Q-ICS-205-930 from 5-HT3 recognition sites in rat brain membranes | B | 8.71 | pIC50 | 1.95 | nM | IC50 | J Med Chem (1992) 35: 1019-1031 [PMID:1552497] |
| ChEMBL | Concentration required to inhibit the binding of radioligand [3H]GR-65630 to serotonin 5-hydroxytryptamine-3 receptor (5-HT 3 receptor)in rat brain cortical membrane | B | 8.81 | pIC50 | 1.54 | nM | IC50 | J Med Chem (2003) 46: 702-715 [PMID:12593651] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 receptor in rat cortical membrane using [3H]GR-65630 as radioligand | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 619-624 [PMID:9871571] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 3 receptor by displacement of [3H]2 in Neuroblastoma-Glioma NG-108-15 cells | B | 7.79 | pKi | 16.2 | 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 | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1990) 33: 2721-2725 [PMID:2145434] |
| ChEMBL | Binding affinity to human HT3A receptor | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6538-6541 [PMID:20889341] |
| ChEMBL | Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by filter binding assay | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| ChEMBL | Antagonist activity at human 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method | F | 10.05 | pIC50 | 0.09 | nM | IC50 | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563] | ||||||||
| ChEMBL | Displacement of [3H]LY 278584 from 5-HT3 receptor in Sprague-Dawley rat cerebral cortex after 30 mins | B | 9.11 | pKi | 0.77 | nM | Ki | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Antagonist activity at rat 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method | F | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| Serotonin 3a (5-HT3a) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3666] [UniProtKB: O70212] | ||||||||
| ChEMBL | Antagonist activity at 5HT3 receptor in guinea pig ileum longitudinal muscle myenteric plexus assessed as inhibition of 2-methyl-5-HT-induced contraction | F | 6.9 | pKd | 125.89 | nM | Kd | Bioorg Med Chem Lett (2010) 20: 6773-6776 [PMID:20851599] |
| ChEMBL | Antagonist activity at 5-HT3 receptor in guinea pig ileum muscle | F | 6.9 | pKd | 125.89 | nM | Kd | Bioorg Med Chem Lett (2011) 21: 1253-1256 [PMID:21256009] |
| ChEMBL | Antagonist activity at 5-HT3 receptor in guinea-pig ileum assessed as inhibition of 5HT-induced contraction incubated for 15 mins | B | 7.11 | pKd | 77.62 | nM | Kd | J Med Chem (2021) 64: 13279-13298 [PMID:34467765] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand. | B | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| ChEMBL | In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1999) 42: 5020-5028 [PMID:10585211] |
| 5-ht5b receptor/Serotonin 5b (5-HT5b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2619] [GtoPdb: 648] [UniProtKB: P35365] | ||||||||
| ChEMBL | The binding affinity was measured on tryptamine receptor using [3H]- tryptamine as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of SERT-mediated [3H]5HT uptake in rat synaptosomes by scintillation counting | B | 5.7 | pIC50 | >2000 | nM | IC50 | J Med Chem (2011) 54: 3206-3221 [PMID:21486038] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | The binding affinity was measured on sigma receptor using [3H]- (+)-3-PPP as radioligand. | B | 6.17 | pKi | 680 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.69 | pIC50 | 20400 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.76 | pIC50 | 17400 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| TRH1 receptor/Thyrotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4553] [GtoPdb: 363] [UniProtKB: Q01717] | ||||||||
| ChEMBL | The binding affinity was measured on TRH receptor using [3H]- MeTRH as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3693-3699 [PMID:8246239] |
| 5-HT3AB in Human [GtoPdb: 378] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
| 5-HT3A in Human [GtoPdb: 379] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | ~5 | nM | Ki |
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620]; Neuropharmacology (2001) 41: 282-4 [PMID:11489465]; Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349] |
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]
