ketanserin [Ligand Id: 88] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL51 (Ketanserin, Ketanserin tartrate, KJK 945, NSC-758959, Perketan, R-41,468, R-41468, R 49945, R-49945, Serepress, Sufrexal)
  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728]
  • 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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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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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 Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
  • 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 Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • Serotonin 2a (5-HT2a) receptor in Pig [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940]
  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Mouse [ChEMBL: CHEMBL4295886] [GtoPdb: 1012] [UniProtKB: Q8BRU6]
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  • Vesicular acetylcholine transporter in Rat [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
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  • α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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  • Vesicular monoamine transporter 1 in Human [GtoPdb: 1011] [UniProtKB: P54219]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
GtoPdb - - 8.2 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
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 in Human [GtoPdb: 214] [UniProtKB: P21728]
GtoPdb - - 6.7 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
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]
GtoPdb - - 5 pKi - - - Biochem J (1992) 285 ( Pt 3): 933-8 [PMID:1386736]
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]
GtoPdb - - 5.4 pIC50 - - - Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569];
Br J Pharmacol (1998) 123: 1655-65 [PMID:9605573]
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
GtoPdb - - 8.3 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407]
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]
GtoPdb - - 7.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
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]
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]
GtoPdb - - 9.7 pKi 0.2 nM Ki Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Life Sci (1996) 59: 1259-68 [PMID:8845011];
Life Sci (2003) 73: 193-207 [PMID:12738034]
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]
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