Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL46 (A04AA01, Desmethylondansetron, EUR-1025, GR-38032, GR-38032F, NSC-757870, Ondansetron, Zofran, Zofran odt, Zuplenz) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]