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

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: CHEMBL51 (Ketanserin, Ketanserin tartrate, KJK 945, NSC-758959, Perketan, R-41468, R-41,468, R 49945, R-49945, Serepress, Sufrexal)
  • D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • Vesicular acetylcholine transporter in Rat [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
There should be some charts here, you may need to enable JavaScript!
  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368]
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
There should be some charts here, you may need to enable JavaScript!
  • Vesicular monoamine transporter 1 in Human [GtoPdb: 1011] [UniProtKB: P54219]
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
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 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
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 Antagonist activity at 5HT2A receptor F 8.7 pKi 2 nM Ki J. Med. Chem. (2012) 55: 5749-5759 [PMID:22694093]
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 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 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]
GtoPdb - - 9 pKi - - - Mol Pharmacol (2000) 58: 877-86 [PMID:11040033];
J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
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 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 Binding affinity to 5HT2A receptor in Sprague-Dawley rat frontal cortical homogenates after 15 mins B 9.07 pKi 0.85 nM Ki