risperidone [Ligand Id: 96] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL85 (LY-03004, LY03004, N05AX08, NSC-759895, 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) |
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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 | 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] |
| 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 | 7.85 | pKi | 14 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
