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

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ChEMBL ligand: CHEMBL2103778 (Cilansetron, KC-9946)
  • 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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  • 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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  • 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-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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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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  • 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
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 5 pKi >10000 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]
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]
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]
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 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]
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 5.07 pKi 8500 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]
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 pKi >10000 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 5 pKi >10000 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
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 5.31 pKi 4900 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]
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 6.02 pKi 960 nM Ki J Med Chem (1993) 36: 3693-3699 [PMID:8246239]
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]
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 6.47 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 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]