cilansetron [Ligand Id: 2297] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103778 (Cilansetron, KC-9946)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-ht5b receptor/5-hydroxytryptamine receptor 5B in Rat [ChEMBL: CHEMBL2619] [GtoPdb: 648] [UniProtKB: P35365]
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  • α2A-adrenoceptor/Alpha-2A adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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  • CCK1 receptor/Cholecystokinin receptor type A in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
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  • D1 receptor/D(1A) dopamine receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/D(3) dopamine receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • δ receptor/Delta-type opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • CCK2 receptor/Gastrin/cholecystokinin type B receptor in Rat [ChEMBL: CHEMBL3508] [GtoPdb: 77] [UniProtKB: P30553]
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  • GluN2C/Glutamate receptor ionotropic, NMDA 2C in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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  • glycine receptor α4 subunit (pseudogene in humans)/Glycine receptor subunit alpha-4 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 subunit alpha in Rat [ChEMBL: CHEMBL4289] [GtoPdb: 1708] [UniProtKB: P22273]
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  • κ receptor/Kappa-type 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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  • 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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  • μ receptor/Mu-type opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • TRH1 receptor/Thyrotropin-releasing hormone receptor in Rat [ChEMBL: CHEMBL4553] [GtoPdb: 363] [UniProtKB: Q01717]
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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
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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 pKi >10000 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
5-HT1D receptor/5-hydroxytryptamine receptor 1D 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 5 pKi >10000 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
5-HT2C receptor/5-hydroxytryptamine receptor 2C 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 5.31 pKi 4900 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
5-HT4 receptor/5-hydroxytryptamine receptor 4 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 6.02 pKi 960 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
5-ht5b receptor/5-hydroxytryptamine receptor 5B 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]
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 receptor type A 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]
D1 receptor/D(1A) dopamine 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/D(2) dopamine 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]
D3 receptor/D(3) dopamine 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]
δ receptor/Delta-type 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]
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]
CCK2 receptor/Gastrin/cholecystokinin type 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 5 pKi >10000 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
GluN2C/Glutamate receptor ionotropic, NMDA 2C 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 subunit alpha-4 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]
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 5.19 pKi 6500 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 subunit alpha 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-type 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]
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 6.04 pKi 910 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]
μ receptor/Mu-type 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 5.07 pKi 8500 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
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-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes B 5.25 pKi 5600 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 9.72 pKi 0.19 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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 6.47 pKi 340 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
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-HT3A in Human [GtoPdb: 379]
GtoPdb - - 9.3 pKi - - - J Pharmacol Sci (2007) 104: 263-73 [PMID:17652911]

ChEMBL data shown on this page come from version 36:

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]