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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) |
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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 32:
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]