ritanserin [Ligand Id: 97] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267777 (NSC-758470, R 55,667, R-55667, Ritanserin, Tiserton)
  • 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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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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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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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 - - 8.4 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 Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes B 7.33 pIC50 47 nM IC50 J. Med. Chem. (1992) 35: 4813-4822 [PMID:1336053]
ChEMBL Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor B 7.33 pIC50 47 nM IC50 J. Med. Chem. (1992) 35: 4823-4831 [PMID:1336054]
ChEMBL Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes B 7.33 pIC50 47 nM IC50 J. Med. Chem. (1996) 39: 3723-3738 [PMID:8809161]
Diacylglycerol kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105787] [UniProtKB: P23743]
ChEMBL Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis B 4.78 pIC50 16700 nM IC50 Eur J Med Chem (2019) 164: 378-390 [PMID:30611057]
ChEMBL Inhibition of FLAG-tagged DGKa (unknown origin) using lipids and [gamma-32P]-ATP incubated for 15 mins by scintillation counting method B 5.05 pIC50 9000 nM IC50 WO-2017177037-A1. Compositions and methods for treating cancer (null)
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity against dopamine receptor D2 from rat corpus striatum by using radioligand [3H]sulpiride B 7.03 pKi 93 nM Ki J. Med. Chem. (1993) 36: 1488-1495 [PMID:8496917]
ChEMBL In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement. B 7.33 pKi 47 nM Ki J. Med. Chem. (1993) 36: 3073-3076 [PMID:7901415]
ChEMBL Binding constant against dopamine receptor D2 (in vitro) B 7.66 pKi 22 nM Ki J. Med. Chem. (1991) 34: 2477-2483 [PMID:1908521]
ChEMBL The compound was tested for its binding affinity towards Dopamine receptor D2 by displacing [3H]5-HT radioligand in rat cerebral cortex B 8.52 pKi 3 nM Ki J. Med. Chem. (1992) 35: 552-558 [PMID:1346653]
ChEMBL The concentration required to inhibit [3H]spiperone binding to dopamine receptor D2 in rat brain membranes (in vitro) B 7.64 pIC50 23 nM IC50 J. Med. Chem. (1991) 34: 2477-2483 [PMID:1908521]
ChEMBL Compound was tested for the displacement of [3H]spiperone from dopamine receptor D2 from rat striatal membranes. B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1992) 35: 4813-4822 [PMID:1336053]
ChEMBL Inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat striatal membranes B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1988) 31: 2247-2256 [PMID:2903929]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptors in rat striatal membranes B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1993) 36: 2761-2770 [PMID:8410990]
ChEMBL Binding affinity at dopamine D2 receptor by [3H]spiperone displacement. B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1994) 37: 950-962 [PMID:8151622]
ChEMBL Binding affinity to dopamine receptor D2 using a [3H]-spiperone binding assay in rat cortical membranes B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1996) 39: 3723-3738 [PMID:8809161]
ChEMBL Compound was tested for the displacement of [3H]spiperone from dopamine receptor D2 B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1992) 35: 4823-4831 [PMID:1336054]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Binding constant against histamine H1 receptor (in vitro) B 8.22 pKi 6 nM Ki J. Med. Chem. (1991) 34: 2477-2483 [PMID:1908521]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
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 6.6 pKd 251.19 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
GtoPdb - - 5.5 pIC50 - - - Life Sci (1997) 60: 653-65 [PMID:9048968]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding constant against 5-hydroxytryptamine 1A receptor (in vitro) B 6 pKi 1000 nM Ki J. Med. Chem. (1991) 34: 2477-2483 [PMID:1908521]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) B 9.35 pKi 0.45 nM Ki Eur J Med Chem (2019) 164: 378-390 [PMID:30611057]
GtoPdb - - 9.4 pKi - - - Br J Pharmacol (1999) 126: 572-4 [PMID:10188965]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]MDL100907 from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy B 7.44 pKi 36 nM Ki Bioorg. Med. Chem. (2008) 16: 4661-4669 [PMID:18296055]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. (2008) 16: 4661-4669 [PMID:18296055]
ChEMBL Binding affinity was evaluated in vitro by displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor on rat cortical membrane B 9.2 pKi 0.63 nM Ki J. Med. Chem. (1997) 40: 586-593 [PMID:9046349]
GtoPdb - - 9.2 pKi - - - Mol Pharmacol (2000) 58: 877-86 [PMID:11040033];
Br J Pharmacol (1999) 126: 572-4 [PMID:10188965]
ChEMBL In vitro binding affinity towards serotonin 5-HT2A receptor in rat cortical membranes using [3H]ketanserin as radioligand B 8.77 pIC50 1.7 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 415-420
ChEMBL Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (1996) 39: 3723-3738 [PMID:8809161]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]LSD from human 5HT2C receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method B 8.72 pKi 1.9 nM Ki MedChemComm (2018) 9: 1069-1075 [PMID:30108996]
ChEMBL Displacement of [3H]mesulergine from human recombinant 5-HT2C receptor expressed in Flp-IN HEK cell membrane after 90 mins by scintillation counting method B 8.74 pKi 1.8 nM Ki MedChemComm (2015) 6: 601-605
ChEMBL Displacement of [3H]mesulergine from human 5-HT2C receptor measured after 90 mins by microbeta scintillation counting method B 8.74 pKi 1.8 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 3216-3219 [PMID:27261181]
ChEMBL Binding affinity to 5HT2C receptor (unknown origin) B 9.15 pKi 0.71 nM Ki Eur J Med Chem (2019) 164: 378-390 [PMID:30611057]
GtoPdb - - 9.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor B 7.35 pKi 45 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 7.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657];
J Biol Chem (1993) 268: 23422-6 [PMID:8226867]
ChEMBL Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor B 7.8 pKi 15.85 nM Ki J. Med. Chem. (2003) 46: 5638-5650 [PMID:14667218]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards 5-hydroxytryptamine 7 receptor B 7.8 pKi 15.85 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1097-1100 [PMID:10843226]
GtoPdb - - 7.8 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 7.82 pKi 15 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.5 pIC50 - - - Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 328-34 [PMID:9303569];
Br J Pharmacol (1998) 123: 1655-65 [PMID:9605573]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.6 pKi - - - Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 9.2 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Br J Pharmacol (1999) 126: 572-4 [PMID:10188965];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568];
Br J Pharmacol (1999) 127: 1075-82 [PMID:10455251]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 8.3 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
GtoPdb - - 7.6 pKi - - - Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 7.4 pKi - - - Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.4 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.8 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J Neurochem (1998) 71: 2169-77 [PMID:9798944];
Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]
α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368]
GtoPdb - - 8 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb - - 7.8 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]