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)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
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  • CCK2 receptor/Cholecystokinin B receptor in Rat [ChEMBL: CHEMBL3508] [GtoPdb: 77] [UniProtKB: P30553]
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  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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  • glycine receptor α4 subunit (pseudogene in humans)/Glycine receptor alpha-4 chain in Mouse [ChEMBL: CHEMBL3500] [GtoPdb: 426] [UniProtKB: Q61603]
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  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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  • Interleukin-6 receptor, α subunit/Interleukin-6 receptor alpha chain in Rat [ChEMBL: CHEMBL4289] [GtoPdb: 1708] [UniProtKB: P22273]
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  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
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  • BLT1 receptor/Leukotriene B4 receptor 1 in Rat [ChEMBL: CHEMBL2126] [GtoPdb: 267] [UniProtKB: Q9R0Q2]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Mouse [ChEMBL: CHEMBL3365] [GtoPdb: 468] [UniProtKB: P49582]
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
  • Serotonin 3a (5-HT3a) receptor in Guinea pig [ChEMBL: CHEMBL3666] [UniProtKB: O70212]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-ht5b receptor/Serotonin 5b (5-HT5b) receptor in Rat [ChEMBL: CHEMBL2619] [GtoPdb: 648] [UniProtKB: P35365]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
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  • TRH1 receptor/Thyrotropin-releasing hormone receptor in Rat [ChEMBL: CHEMBL4553] [GtoPdb: 363] [UniProtKB: Q01717]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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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 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 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-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]
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 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]