[3H]ketanserin [Ligand Id: 197] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL51 (Ketanserin, Ketanserina, Ketanserine, Ketanserin tartrate, KJK 945, NSC-758959, Perketan, R-41,468, R-41468, R 49945, R-49945, Serepress, Sufrexal) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vitro binding affinity towards dDopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate | B | 5.52 | pKi | >3000 | nM | Ki | J Med Chem (1989) 32: 1431-1435 [PMID:2525621] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone | B | 6.62 | pKi | 240 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand | B | 6.31 | pKi | 491 | nM | Ki | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
| ChEMBL | Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane | B | 6.44 | pKi | 359 | nM | Ki | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Binding affinity to rat striatum homogenate membrane D2 receptor incubated for 10 mins | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat striatal membranes | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (1988) 31: 2247-2256 [PMID:2903929] |
| ChEMBL | Binding affinity at dopamine D2 receptor by [3H]spiperone displacement. | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (1994) 37: 950-962 [PMID:8151622] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Binding affinity towards human dopamine receptor D4 | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Antagonist activity at histamine H1 receptor | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2012) 55: 5749-5759 [PMID:22694093] |
| Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
| ChEMBL | Antagonism against H1 histamine receptor of guinea pig ileum | F | 8.85 | pKd | 1.41 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 667-672 |
| ChEMBL | Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Displacement of [125I]RTI-55 from human NET expressed in HEK293 cell membranes | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 6.1 | pKd | 794.33 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampus | B | 5.71 | pKi | 1933 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1229-1231 [PMID:11354383] |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 5.72 | pKi | 1900 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain | B | 5.74 | pKi | 1817 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| ChEMBL | Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
| ChEMBL | The compound was evaluated for the ability to displace [3H]- 8-OH -DPAT from 5-hydroxytryptamine 1A receptor ( striata of male wistar rats) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2457-2461 [PMID:11078200] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1999) 42: 4981-5001 [PMID:10585208] |
| ChEMBL | Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. | B | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (1997) 40: 3497-3500 [PMID:9357514] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 5.72 | pKi | 1900 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (1999) 42: 4981-5001 [PMID:10585208] |
| ChEMBL | Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (1997) 40: 3497-3500 [PMID:9357514] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 9.7 | pKd | 0.2 | nM | Kd |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Life Sci (2003) 73: 193-207 [PMID:12738034] |
| ChEMBL | Displacement of [125I]DOI from human 5HT2A receptor expressed in HEK293 cell membranes | B | 7.97 | pKi | 10.7 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Inhibition of 5-HT2A (unknown origin) assessed as inhibition constant | B | 8.43 | pKi | 3.71 | nM | Ki | Eur J Med Chem (2018) 151: 628-685 [PMID:29656203] |
| ChEMBL | Antagonist activity at 5HT2A receptor | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2012) 55: 5749-5759 [PMID:22694093] |
| ChEMBL | Antagonist activity at 5-HT2A (unknown origin) assessed as inhibition constant | F | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2021) 211: 113016-113016 [PMID:33243532] |
| ChEMBL | Displacement of radiolabeled ketanserin from human 5HT2A receptor | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity to human 5-HT2A receptor by radioligand displacement assay | B | 9.31 | pKi | 0.49 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H] ketanserin from human recombinant 5-HT2A receptor measured after 60 mins by scintillation counter method | B | 9.35 | pKi | 0.45 | nM | Ki | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor expressed in NIH3T3 cells | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2008) 51: 6808-6828 [PMID:18847250] |
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-293 cells | B | 9.52 | pKi | 0.3 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEK293 cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2011) 54: 5320-5334 [PMID:21726069] |
| ChEMBL | Displacement of [3H]ketanserein from 5HT2A receptor F340L mutant expressed in NIH3T3 cells | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (2008) 51: 6808-6828 [PMID:18847250] |
| ChEMBL | Antagonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay | F | 7.08 | pIC50 | 83.7 | nM | IC50 | J Med Chem (2018) 61: 10017-10039 [PMID:30383372] |
| ChEMBL | Antagonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
| ChEMBL | Antagonist activity at human 5HT2A receptor expressed in EC80 serotonin-stimulated CHOK1 cells by calcium mobilization assay | F | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2530-2532 [PMID:19328689] |
| ChEMBL | Antagonist activity at human 5-HT2A receptor assessed as inhibition of 5-HT-mediated internal calcium mobilization by FLIPR assay | F | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5102-5106 [PMID:26475518] |
| ChEMBL | Antagonist activity at human 5HT2A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay | F | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
| ChEMBL | Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| ChEMBL | Inhibition of human 5HT2A receptor | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method | F | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Inhibition of human 5-HT2A receptor | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Displacement of radiolabeled ketanserin from human 5HT2A receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity to human 5-HT2A receptor by radioligand displacement assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H] ketanserin from human recombinant 5-HT2A receptor measured after 60 mins by scintillation counter method | B | 9.09 | pIC50 | 0.82 | nM | IC50 | Eur J Med Chem (2019) 176: 292-309 [PMID:31112891] |
| ChEMBL | Binding affinity to human 5-HT2A receptor by radioligand displacement assay | B | 9.11 | pIC50 | 0.77 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting | B | 9.28 | pIC50 | 0.52 | nM | IC50 | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEK293 cells | B | 9.46 | pIC50 | 0.35 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method | B | 9.46 | pIC50 | 0.35 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay | F | 8.98 | pEC50 | 1.04 | nM | EC50 | Eur J Med Chem (2013) 63: 558-569 [PMID:23537943] |
| Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129] | ||||||||
| ChEMBL | Antagonist activity at serotonin 5HT2A receptor assessed as effect on 5HT-induced isometric contractile force in isolated rings of pig coronary artery | F | 8.88 | pKd | 1.32 | nM | Kd | Bioorg Med Chem Lett (2008) 18: 3809-3813 [PMID:18534847] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 8.8 | pKd | - | - | - | Mol Pharmacol (2000) 58: 877-86 [PMID:11040033] |
| ChEMBL | Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta | F | 8.87 | pKd | 1.35 | nM | Kd | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
| ChEMBL | Antagonism of 5-HT2A receptor of rat tail artery | F | 9.55 | pKd | 0.28 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 667-672 |
| ChEMBL | Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex | B | 8.29 | pKi | 5.13 | nM | Ki | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley cortex membrane | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Displacement of [3H]DOI-HCL from 5HT2A in Sprague-Dawley rat frontal cortex membranes measured after 20 mins | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| ChEMBL | Binding affinity to rat frontal cortex homogenate membrane 5-HT2A receptor incubated for 10 mins | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| ChEMBL | Displacement of [3H]ketanserin from Sprague-Dawley rat 5-HT2A receptor assessed as inhibition constant measured after 60 mins by competitive binding assay | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem (2023) 96: 117518-117518 [PMID:37951135] |
| ChEMBL | Displacement of [3H]- Ketanserin from rat cortex 5-hydroxytryptamine 2A receptor | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1229-1231 [PMID:11354383] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A in Sprague-Dawley rat frontal cortex membranes measured after 20 mins | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex incubated for 15 mins by liquid scintillation counting analysis | B | 9.07 | pKi | 0.85 | nM | Ki | Eur J Med Chem (2016) 110: 133-150 [PMID:26820556] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex incubated for 15 mins | B | 9.07 | pKi | 0.85 | nM | Ki | Eur J Med Chem (2016) 116: 173-186 [PMID:27061981] |
| ChEMBL | Binding affinity to 5HT2A receptor in Sprague-Dawley rat frontal cortical homogenates after 15 mins | B | 9.07 | pKi | 0.85 | nM | Ki | Eur J Med Chem (2011) 46: 2206-2216 [PMID:21440338] |
| ChEMBL | Displacement of [3H]ketanserin from serotonin 5-HT2A receptor in Sprague-Dawley rat brain cortex homogenates incubated for 15 mins by liquid scintillation spectrometry | B | 9.07 | pKi | 0.85 | nM | Ki | Bioorg Med Chem (2017) 25: 5820-5837 [PMID:28943244] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A in Sprague-Dawley rat brain cortex by liquid scintillation counting | B | 9.07 | pKi | 0.85 | nM | Ki | Eur J Med Chem (2010) 45: 752-759 [PMID:19954866] |
| ChEMBL | Displacement of [3H]ketanserin from Sprague-Dawley rat brain cortex serotonin 5-HT2A receptor after 15 mins by liquid scintillation counting | B | 9.07 | pKi | 0.85 | nM | Ki | Eur J Med Chem (2012) 47: 520-529 [PMID:22133459] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex membrane | B | 9.31 | pKi | 0.49 | nM | Ki | Bioorg Med Chem (2007) 15: 7581-7589 [PMID:17900912] |
| ChEMBL | Displacement of [3H]ketanserin from 5-HT2A receptor in Sprague-Dawley rat frontal cortex after 15 mins | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (2013) 56: 7851-7861 [PMID:24050112] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins | B | 6.74 | pKi | 180 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins | B | 6.54 | pIC50 | 290 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus | B | 7.36 | pKi | 43.65 | nM | Ki | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
| ChEMBL | Percent inhibition against 5-hydroxytryptamine 2C receptor at 1 uM | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1C receptor in rat using [3H]mesulergine as radioligand | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1992) 35: 4903-4910 [PMID:1479590] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 4.7 | pKi | 20000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | B | 4.7 | pKi | 20000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 5.55 | pKi | 2800 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 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-HT from human 5-hydroxytryptamine 7 receptor | B | 5.87 | pKi | 1334 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 5.9 | pKi | 1258.93 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cell membranes | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | The compound was tested for affinity towards sigma-3 receptor | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940] | ||||||||
| ChEMBL | Displacement of [3H](+)-syn-Ethyl 1-(2-(2,4-Dioxo-1,2-dihydroquinazolin-3(4H)-yl)ethyl)-4-(4-fluorophenyl)piperidine-3-carboxylate from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | B | 5.92 | pKi | 1190 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Displacement of [3H]reserpine from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Displacement of [3H]DHTB from human VMAT2 expressed in HEK293 cell membranes incubated for 90 mins by microbeta scintillation counting method | B | 7.11 | pKi | 77 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Inhibition of human VMAT2 expressed in HEK293 cell membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 6 mins | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295886] [GtoPdb: 1012] [UniProtKB: Q8BRU6] | ||||||||
| ChEMBL | Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666] | ||||||||
| ChEMBL | Displacement of [125I]O-iodo-trans-decalinvesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 1 hr by gamma counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
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]
