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) |
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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/Diacylglycerol kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105787] [GtoPdb: 3256] [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] |
| TAS2R20 in Human [GtoPdb: 671] [UniProtKB: P59543] | ||||||||
| GtoPdb | - | - | 5.22 | pEC50 | 6000 | nM | EC50 | Molecules (2015) 20: 18907-22 [PMID:26501253] |
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]
