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 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)
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]
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 - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]
GtoPdb - - 7 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]