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 Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 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 Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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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 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 Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constant B 8.6 pKi 2.5 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
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]