quetiapine [Ligand Id: 50] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL716 (Atrolak xl, Biquelle xl, Brancico xl, Ebesque xl, Mintreleq xl, Norsic, NSC-758918, Psyquet xl, Quetiapine, Quetiapine extended release, Seotiapim xl, Seroquel, Seroquel xl, Sondate xl, Tenprolide xl, Zaluron xl)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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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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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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]
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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-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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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-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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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-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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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]
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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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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.7 pKi 20 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.46 pKi 34.9 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.06 pIC50 86.2 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 7.87 pKi 13.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 7.61 pIC50 24.5 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.32 pKi 47.5 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.02 pIC50 96.6 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.03 pKi 934.3 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.6 pIC50 2491.4 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Binding affinity to adrenergic alpha2B receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.34 pKi 45.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7 pIC50 100.3 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.21 pKi 61.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.38 pIC50 420.8 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity towards human Dopamine receptor D1 B 5.37 pKi 4240 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned dopamine D1 receptor B 5.89 pKi 1300 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity against dopamine receptor D1 B 6.41 pKi 390 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.67 pKi 214.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.37 pIC50 429.3 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.35 pKi 443.3 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6.4 pKi 400 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding affinity towards human Dopamine receptor D2 B 6.51 pKi 310 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method B 6.51 pKi 309.03 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL Binding affinity to human cloned dopamine D2 receptor B 6.74 pKi 180 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to human dopamine D2 receptor B 6.85 pKi 140 nM Ki Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL Binding affinity towards human D2 dopamine receptor. B 7.16 pKi 69 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL In vitro binding affinity for Dopamine receptor D2 B 7.2 pKi 63.1 nM Ki Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
GtoPdb - - 7.2 pKi 69 nM Ki Neuropsychopharmacology (1998) 18: 63-101 [PMID:9430133]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.88 pIC50 1329.9 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum tissue after 20 mins by scintillation counting B 6.74 pKi 180 nM Ki Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL Inhibition of spiropiperidone binding at dopamine receptor D2 of rat. B 6.48 pIC50 330 nM IC50 J Med Chem (2001) 44: 372-389 [PMID:11462978]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity towards human Dopamine receptor D3 B 6.19 pKi 650 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.4 pKi 395.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human dopamine receptor D3 B 6.47 pKi 340 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to human cloned dopamine D3 receptor B 6.49 pKi 320 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 6.6 pKi 251.19 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.93 pIC50 1163.2 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity to human cloned dopamine D4 receptor B 5.66 pKi 2200 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity towards human dopamine-4.2 receptor B 5.8 pKi 1600 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity towards human dopamine receptor D4 B 5.8 pKi 1600 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting B 6 pKi >1000 nM Ki J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of hERG K channel F 5.24 pIC50 5800 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human ERG B 5.24 pIC50 5754.4 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity towards human H1 receptor B 7.68 pKi 21 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity towards human histamine H1 receptor B 7.72 pKi 19 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to H1 histamine receptor (unknown origin) B 7.96 pKi 11 nM Ki Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775]
ChEMBL Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay B 8 pKi 10 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity to human cloned histamine H1 receptor B 8.06 pKi 8.7 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.34 pKi 4.6 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.7 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.4 pIC50 39.6 nM IC50 DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Displacement of [3H]mepyramine from H1R in rat brain B 7.4 pIC50 40 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum B 7.4 pKi 39.81 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
Histone H1.0 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707465] [UniProtKB: P07305]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8 pKi 10 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to M1 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.2 pKi 629.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells B 6.4 pKi 398.11 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor B 7 pKi 100 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity towards human M1 receptor. B 7.25 pKi 56 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.58 pIC50 2615 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells F 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.92 pKi 1189.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to M2 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.48 pIC50 3344.7 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Binding affinity to M3 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Binding affinity to M4 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.66 pKi 220.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells B 6.9 pKi 125.89 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.8 pIC50 1578.7 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.67 pKi 2155.9 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to M5 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.52 pIC50 3000.7 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1 receptor B 6.08 pKi 830 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in human brain tissue incubated for 30 mins by scintillation counting analysis B 6.52 pKi 300 nM Ki Bioorg Med Chem Lett (2019) 29: 126679-126679 [PMID:31537425]
GtoPdb - - 6.6 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039];
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity to human cloned 5HT1A receptor B 6.64 pKi 230 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to human 5HT1A receptor B 6.74 pKi 180 nM Ki Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting B 6.9 pKi 125 nM Ki J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 7.1 pKi 79.43 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.09 pKi 815.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting B 6.64 pKi 230 nM Ki Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.85 pIC50 1426.4 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 5.7 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 5.9 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity to serotonin 5-HT1E receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity to human 5HT2A receptor B 6.66 pKi 220 nM Ki Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL Binding affinity to human cloned 5HT2A receptor B 6.66 pKi 220 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6.69 pKi 202 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method B 6.92 pKi 120.23 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor B 6.92 pKi 120 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting B 7 pKi 101 nM Ki J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
GtoPdb - - 7 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
GtoPdb - - 7 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 7.09 pKi 82 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells B 7.2 pKi 63.1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.47 pKi 33.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Ketanserin from 5-HT2A receptor in human brain tissue incubated for 60 mins by scintillation counting analysis B 7.51 pKi 31 nM Ki Bioorg Med Chem Lett (2019) 29: 126679-126679 [PMID:31537425]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.93 pIC50 117.8 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting B 6.66 pKi 220 nM Ki Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells B 6.6 pKi 251.19 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.87 pKi 135.9 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.67 pIC50 213.5 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor B 5.42 pKi 3820 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 5.7 pKi 2000 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.76 pKi 1729 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human 5-hydroxytryptamine 2C receptor B 5.82 pKi 1500 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to human cloned 5HT2C receptor B 5.85 pKi 1400 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.48 pIC50 3300.8 nM IC50 DrugMatrix in vitro pharmacology data
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to serotonin 5-HT3 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity to human cloned 5HT6 receptor B 5.85 pKi 1400 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 7.2 pKi 63.1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding affinity to human SERT B 4.74 pKi >18000 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6 pKi >1000 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.02 pKi 963.9 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.64 pIC50 2293.5 nM IC50 DrugMatrix in vitro pharmacology data
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA F 4.77 pIC50 16900 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Binding affinity to rat NET B 6.17 pKi 680 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes F 4.98 pIC50 10400 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 4.98 pIC50 10400 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 5.6 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 6.03 pKi 927 nM Ki Neuropsychopharmacology (2008) 33: 2303-12 [PMID:18059438]

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]