risperidone [Ligand Id: 96] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL85 (LY-03004, LY03004, N05AX08, NSC-759895, Okedi, Perseris, Perseris kit, R 64 766, R-64,766, R-64-766, R-64766, RCN-3028, RCN3028, Risperdal, Risperdal consta, Risperdal Consta Long Acting, Risperdal M, Risperdal M-Tab, Risperdal quicklet, Risperidone, Rykindo, Uzedy)
  • 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]
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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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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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Mouse [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
  • 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]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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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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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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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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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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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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  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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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 Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
  • 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]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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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]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • 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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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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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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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 8 pKi 10 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active B 8.55 pKi 2.8 nM Ki Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8.64 pKi 2.3 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
GtoPdb - - 8.7 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
ChEMBL Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay F 7.96 pIC50 10.9 nM IC50 Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
ChEMBL Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay F 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding. B 7.89 pKi 13 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine. B 9.06 pKi 0.88 nM Ki US-8802672-B2. Pyrimidinyl-piperazines useful as D3/D2 receptor ligands (2014)
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 9.4 pKi 0.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 9 pIC50 0.99 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]
GtoPdb - - 8 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
ChEMBL Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay B 8 pKi 10 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 8.97 pKi 1.08 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.71 pIC50 1.95 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]
GtoPdb - - 7.4 pKi - - - Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.31 pKi 4.91 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8 pIC50 9.99 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
GtoPdb - - 7.3 pKi - - - Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL Binding affinity to alpha2 adrenergic receptor (unknown origin) B 7.55 pKi 28.2 nM Ki Bioorg Med Chem Lett (2020) 30: 127506-127506 [PMID:32828898]
ChEMBL Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor B 8 pKi 10 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.44 pKi 3.63 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.01 pIC50 9.67 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding. B 7.6 pKi 25 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
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 7.92 pKi 12 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.59 pIC50 26 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 8 pKi 10 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor B 8.49 pKi 3.2 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 8.86 pKi 1.39 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 8.02 pIC50 9.56 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding. B 4.66 pKi 22000 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.28 pIC50 5273.4 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 to dopamine D1 receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity towards human Dopamine receptor D1 B 6.21 pKi 620 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned dopamine D1 receptor B 6.24 pKi 580 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.62 pKi 240 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor B 6.83 pKi 147.91 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Binding affinity against dopamine receptor D1 B 7.68 pKi 21 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.32 pIC50 479 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding. B 6.6 pKi 251 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 B 6.83 pKi 147 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry B 7.3 pKi 50 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Affinity for Dopamine receptor D1 B 7.66 pKi 22 nM Ki Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
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 8 pKi 10 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.18 pKi 6.54 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 B 8.19 pKi 6.4 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells B 8.2 pKi 6.31 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2 receptor B 8.21 pKi 6.17 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay B 8.21 pKi 6.17 nM Ki Medchemcomm (2011) 2: 1194-1200
ChEMBL Displacement of [3H]spiperone from human D2 receptor B 8.21 pKi 6.17 nM Ki Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8.23 pKi 5.9 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) B 8.41 pKi 3.9 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Binding affinity to D2 receptor (unknown origin) B 8.42 pKi 3.8 nM Ki Bioorg Med Chem Lett (2020) 30: 127506-127506 [PMID:32828898]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) B 8.42 pKi 3.8 nM Ki J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL Binding affinity towards human Dopamine receptor D2 B 8.48 pKi 3.3 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity for dopamine receptor D2 determined using [3H]spiperone B 8.51 pKi 3.1 nM Ki Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay B 8.57 pKi 2.7 nM Ki J Med Chem (2012) 55: 9735-9750 [PMID:23043306]
ChEMBL Binding affinity to human cloned dopamine D2 receptor B 8.66 pKi 2.2 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells B 8.85 pKi 1.4 nM Ki J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 9.22 pKi 0.6 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding affinity towards human D2 dopamine receptor. B 9.36 pKi 0.44 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
GtoPdb - - 9.36 pKi 0.44 nM Ki Neuropsychopharmacology (1998) 18: 63-101 [PMID:9430133]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at dopamine D2 receptor (unknown origin) after 60 mins by Ultra lance cAMP assay F 8.15 pIC50 7.09 nM IC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
ChEMBL Inhibition of mouse Dopamine receptor D2 B 7.64 pIC50 23 nM IC50 J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding. B 7.72 pKi 19 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Receptor Binding Assay: D2 receptor binding was determined as described by Creese et al. (Eur. J. Pharmacol., 60:55-66, 1979) on rat brain striatal membrane preparation using [3H]spiperone (0.4-1.3 nM) as ligand. Non-specific binding was determined in the presence of 1 μM (+) butaclamol. B 7.89 pKi 13 nM Ki US-8802672-B2. Pyrimidinyl-piperazines useful as D3/D2 receptor ligands (2014)
ChEMBL In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane. B 8.09 pKi 8.13 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Affinity against Dopamine receptor D2 B 8.09 pKi 8.13 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone B 8.18 pKi 6.65 nM Ki J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL Binding affinity to the dopamine receptor D2L in rat brain membranes B 8.29 pKi 5.1 nM Ki J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry B 8.42 pKi 3.8 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.43 pKi 3.71 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]spiperone from D2 receptor in rat striatum measured after 15 mins by liquid scintillation counting method B 8.43 pKi 3.7 nM Ki Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.43 pKi 3.7 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis B 8.43 pKi 3.7 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum incubated for 30 mins by liquid scintillation counting analysis B 8.43 pKi 3.7 nM Ki Eur J Med Chem (2016) 124: 713-728 [PMID:27639363]
ChEMBL Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum homogenates after 30 mins by liquid scintillation counting B 8.43 pKi 3.7 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting B 8.44 pKi 3.6 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in rat brain B 8.51 pKi 3.1 nM Ki Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum B 8.51 pKi 3.1 nM Ki J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL The binding affinity was measured on dopamine receptor D2 in rat brain tissue B 8.55 pKi 2.8 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting B 8.55 pKi 2.8 nM Ki Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum B 8.55 pKi 2.8 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL Affinity for Dopamine receptor D2 B 8.68 pKi 2.1 nM Ki Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
ChEMBL Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats B 8.74 pKi 1.8 nM Ki Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum. B 7.43 pIC50 37.5 nM IC50 J Med Chem (1995) 38: 1119-1131 [PMID:7707315]
ChEMBL In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum B 7.43 pIC50 37 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL Binding affinity towards Dopamine receptor D2 was determined in rat striatum using [3H]- spiperone as radioligand B 7.43 pIC50 37 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue B 7.52 pIC50 30 nM IC50 J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 B 7.56 pIC50 27.4 nM IC50 J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2 B 8.4 pIC50 4 nM IC50 J Med Chem (1992) 35: 1092-1101 [PMID:1348090]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 7 pKi - - - J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding. B 7.51 pKi 31 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor B 7.79 pKi 16.22 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) B 7.84 pKi 14.3 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Binding affinity towards human dopamine receptor D3 B 7.85 pKi 14 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 7.89 pKi 13 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8 pKi 10 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to human cloned dopamine D3 receptor B 8.02 pKi 9.6 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.09 pKi 8.04 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry B 8.17 pKi 6.7 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) B 8.17 pKi 6.7 nM Ki J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.62 pIC50 24 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Displacement of [3H] 7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle homogenates after 60 mins by liquid scintillation counting B 7.5 pKi 31.9 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle B 7.82 pKi 15.1 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL Receptor Binding Assay: Binding assays were carried out on rat recombinant D3 receptors (Perkin-Elmer, Cat. No. 6110139) expressed in Sf9 cells using [3H]spiperone (0.44-1.49 nM) as ligand and haloperidol (10 μM) for determination of non-specific binding. The assay was performed according to the supplier's assay protocol (Cat. No.: 3110139). B 7.89 pKi 13 nM Ki US-8802672-B2. Pyrimidinyl-piperazines useful as D3/D2 receptor ligands (2014)
ChEMBL Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting B 8 pKi 10.1 nM Ki Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis B 8.01 pKi 9.7 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity towards human dopamine receptor D4 B 7.8 pKi 16 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity towards human dopamine-4.2 receptor B 7.8 pKi 16 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells B 8 pKi 10 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to human cloned dopamine D4 receptor B 8.07 pKi 8.5 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells B 8.15 pKi 7 nM Ki J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding. B 8.21 pKi 6.2 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
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
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay B 6.49 pEC50 320 nM EC50 J Med Chem (2015) 58: 2958-2966 [PMID:25790278]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.46 pKi 3432.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method B 6.04 pKi 920 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.38 pIC50 4190.1 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG B 5.88 pIC50 1330 nM IC50 Bioorg Med Chem Lett (2020) 30: 127027-127027 [PMID:32122737]
ChEMBL Inhibition of human ERG by auomated patch clamp assay B 5.88 pIC50 1330 nM IC50 Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
ChEMBL Inhibition of human ERG B 5.88 pIC50 1330 nM IC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
ChEMBL Inhibition of human ERG after 10 mins B 5.97 pIC50 1070 nM IC50 Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL Inhibition of human ERG B 6.11 pIC50 778 nM IC50 Medchemcomm (2015) 6: 831-838
ChEMBL Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay B 6.24 pIC50 581 nM IC50 J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Inhibitory concentration against IKr potassium channel B 6.59 pIC50 260 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG expressed in HEK293 cells at -50 mV holding potential by patch clamp assay B 6.78 pIC50 167.1 nM IC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Inhibition of human ERG by automated patch method relative to control B 6.78 pIC50 167 nM IC50 Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp method B 6.78 pIC50 167 nM IC50 Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 6.79 pIC50 163 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG in MCF7 cells B 6.79 pIC50 162.18 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 6.79 pIC50 162.18 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.82 pIC50 151.36 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.82 pIC50 151.36 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of hERG K channel F 6.82 pIC50 150 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human ERG channel B 6.83 pIC50 148 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 6.83 pIC50 148 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG B 6.83 pIC50 147.91 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 to H1 histamine receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Binding affinity towards human H1 receptor B 7.06 pKi 88 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor B 7.48 pKi 33 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Binding affinity to H1 histamine receptor (unknown origin) B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775]
ChEMBL Binding affinity to human cloned histamine H1 receptor B 7.72 pKi 19 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
GtoPdb - - 7.8 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.85 pKi 14 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.54 pKi 2.87 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human histamine H1 receptor B 8.59 pKi 2.6 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay B 6.06 pIC50 868 nM IC50 Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay F 6.34 pIC50 454 nM IC50 Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay F 6.34 pIC50 454 nM IC50 Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.6 pIC50 25 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 7.1 pIC50 80 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]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting B 7.34 pKi 46.2 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum B 7.39 pKi 41.2 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting B 7.42 pKi 38.3 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting B 7.64 pKi 22.9 nM Ki Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis B 7.66 pKi 21.7 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum B 8.1 pKi 7.94 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.84 pKi 1458 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.83 pIC50 1483 nM IC50 DrugMatrix in vitro pharmacology data
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to histamine H3 receptor (unknown origin) B 5.96 pKi 1105.5 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 5.8 pIC50 1600 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity towards human M1 receptor. B 5.3 pKi >5000 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor B 5.55 pKi 2800 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to M1 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to M2 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
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
ChEMBL Antagonist activity at M3 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay F 4 pIC50 >100000 nM IC50 Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
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
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Binding affinity to M5 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter B 5.26 pKi >5454 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to 5HT1A receptor B 6.4 pKd 398.11 nM Kd J Med Chem (2009) 52: 6107-6125 [PMID:19754201]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method B 5.93 pKi 1169 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
GtoPdb - - 6.5 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039];
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity to 5HT1A receptor (unknown origin) B 6.57 pKi 271 nM Ki Bioorg Med Chem Lett (2020) 30: 127506-127506 [PMID:32828898]
ChEMBL Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand B 6.6 pKi 253 nM Ki Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 6.6 pKi 251.19 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to human cloned 5HT1A receptor B 6.68 pKi 210 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to 5HT1A receptor (unknown origin) B 6.72 pKi 190 nM Ki J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL Binding affinity to 5-HT1A receptor (unknown origin) B 6.74 pKi 182 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1 receptor B 7.68 pKi 21 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay F 5 pEC50 >10000 nM EC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice. B 6.37 pIC50 430 nM IC50 J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M. B 6.14 pKi 720 nM Ki J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
GtoPdb - - 6.2 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]
ChEMBL Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding. B 6.31 pKi 491 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.34 pKi 457 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex B 6.6 pKi 253 nM Ki J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting B 6.68 pKi 211 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting B 6.72 pKi 190.2 nM Ki Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat brain cortex B 6.72 pKi 190.2 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry B 6.72 pKi 190 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Displacement of [3H](+)8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 30 mins by liquid scintillation counting method B 6.74 pKi 182 nM Ki Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis B 6.74 pKi 182 nM Ki Eur J Med Chem (2016) 124: 713-728 [PMID:27639363]
ChEMBL Displacement of [3H]-8-OH-DPAT from serotonin 5-HT1A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting B 6.74 pKi 181.9 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis B 6.74 pKi 180 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor B 6.89 pKi 130 nM Ki Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus B 6.02 pIC50 950 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand B 6.02 pIC50 950 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue B 6.09 pIC50 820 nM IC50 J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.1 pIC50 799 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]
GtoPdb - - 7.3 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Br J Pharmacol (1998) 123: 1655-65 [PMID:9605573];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay B 8 pKi 10 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]
ChEMBL Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay B 6 pKi 1000 nM Ki Medchemcomm (2012) 3: 580-583
GtoPdb - - 8 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
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 9 pKi <1 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis B 9 pKi 1 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells B 9 pKi 1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor B 9.09 pKi 0.81 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Displacement of [3H]ketanserin from human 5-HT2A receptor B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor B 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay B 9.3 pKi 0.5 nM Ki Medchemcomm (2011) 2: 1194-1200
ChEMBL Displacement of [3H]ketanserin from human cloned 5HT2A receptor B 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor B 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 9.3 pKi 0.5 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 9.41 pKi 0.39 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) B 9.41 pKi 0.39 nM Ki Bioorg Med Chem Lett (2020) 30: 127506-127506 [PMID:32828898]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cell membranes measured after 30 mins B 9.43 pKi 0.37 nM Ki Eur J Med Chem (2019) 180: 673-689 [PMID:31357129]
ChEMBL Binding affinity to human cloned 5HT2A receptor B 9.54 pKi 0.29 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to 5-HT2A receptor (unknown origin) B 9.72 pKi 0.19 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Antagonist activity at 5HT2A receptor (unknown origin) B 9.77 pKi 0.17 nM Ki Eur J Med Chem (2020) 193: 112214-112214 [PMID:32182489]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor B 9.8 pKi 0.16 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) B 9.82 pKi 0.15 nM Ki J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
GtoPdb - - 10 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 10 pKi 0.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay F 8.33 pIC50 4.67 nM IC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
ChEMBL Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay F 9.14 pIC50 0.72 nM IC50 Eur J Med Chem (2019) 180: 673-689 [PMID:31357129]
ChEMBL Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay F 9.15 pIC50 0.71 nM IC50 Eur J Med Chem (2019) 180: 673-689 [PMID:31357129]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 9.46 pIC50 0.35 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]
GtoPdb - - 8.5 pKi - - - J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding. B 9.15 pKi 0.7 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor B 9.27 pKi 0.54 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting B 9.51 pKi 0.31 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex B 9.51 pKi 0.31 nM Ki J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor B 9.51 pKi 0.31 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting B 9.6 pKi 0.25 nM Ki Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex B 9.6 pKi 0.25 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane. B 9.7 pKi 0.2 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Displacement of [3H]ketanserin from rat cerebral cortex 5HT2A receptor measured after 15 mins by liquid scintillation counting method B 9.72 pKi 0.19 nM Ki Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis B 9.74 pKi 0.18 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL Displacement of [3H] ketanserin from 5-HT2A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis B 9.74 pKi 0.18 nM Ki Eur J Med Chem (2016) 124: 713-728 [PMID:27639363]
ChEMBL Displacement of [3H]-ketanserine from serotonin 5-HT2A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting B 9.74 pKi 0.18 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat brain B 9.8 pKi 0.16 nM Ki Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor. B 9.8 pKi 0.16 nM Ki J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry B 9.82 pKi 0.15 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex B 8.59 pIC50 2.6 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor B 8.85 pIC50 1.4 nM IC50 J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells B 7.7 pKi 19.95 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 7.82 pKi 15 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.64 pIC50 23 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 to serotonin 5-HT2C receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus. B 7.04 pKi 91.2 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.2 pKi 63 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor B 7.2 pKi 63 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus B 7.38 pKi 41.69 nM Ki J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor B 7.38 pKi 41.69 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells B 7.48 pKi 33 nM Ki Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL Binding affinity to 5HT2C receptor (unknown origin) B 7.49 pKi 32 nM Ki J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
GtoPdb - - 7.6 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]
ChEMBL Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells B 7.9 pKi 12.59 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor B 7.92 pKi 12 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Binding affinity to human cloned 5HT2C receptor B 8 pKi 10 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 8.12 pKi 7.64 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]mesulergine from human 5HT2C receptor B 8.13 pKi 7.41 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor B 8.13 pKi 7.41 nM Ki Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor B 8.13 pKi 7.41 nM Ki Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 2C receptor B 8.19 pKi 6.4 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.82 pIC50 15 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay F 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay F 8.74 pIC50 1.81 nM IC50 Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex B 6.9 pKi 125.9 nM Ki Medchemcomm (2015) 6: 831-838
ChEMBL Displacement of [3H]mesulergine from 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting B 7.52 pKi 30.1 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Displacement of [3H]-mesulergine from serotonin 5-HT2C receptor in rat brain cerebral cortex homogenates incubated for 15 mins by liquid scintillation counting B 7.55 pKi 28.2 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis B 7.84 pKi 14.5 nM Ki J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
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]
GtoPdb - - 5.6 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
ChEMBL Binding affinity to human cloned 5HT6 receptor B 5.7 pKi 2000 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to 5-HT6 receptor (unknown origin) B 5.88 pKi 1329.2 nM Ki Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method B 5.88 pKi 1329 nM Ki Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis B 5.9 pKi 1260 nM Ki Eur J Med Chem (2016) 124: 713-728 [PMID:27639363]
ChEMBL Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting B 5.9 pKi 1260 nM Ki J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Binding affinity to 5HT6 receptor (unknown origin) B 5.92 pKi 1190 nM Ki Bioorg Med Chem Lett (2020) 30: 127506-127506 [PMID:32828898]
ChEMBL Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 5.96 pKi 1107 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay B 6 pKi >1000 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells B 6.65 pKi 224 nM Ki Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 6.4 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630];
J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
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 8 pKi 10 nM Ki Medchemcomm (2012) 3: 580-583
ChEMBL Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor B 8.37 pKi 4.3 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
GtoPdb - - 8.7 pKi - - - Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958];
Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 9 pKi 1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 9.4 pKi 0.4 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 9 pKd - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630];
J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
ChEMBL Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method B 7.39 pKi 40.7 nM Ki Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting B 8.49 pKi 3.2 nM Ki Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 8.85 pKi 1.4 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding affinity to human SERT B 5.85 pKi 1400 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 Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding. B 5.37 pKi 4300 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay B 4.96 pIC50 11000 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Binding affinity to rat NET B 4.55 pKi 28000 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 4.14 pIC50 73000 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 4.14 pIC50 73000 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 5.9 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]

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]