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ChEMBL ligand: CHEMBL1112 (Abilify, Abilify maintena, Abilify maintena kit, Abilify mycite, Abilify mycite kit, Aripiprazole, Aripiprazole mylan pharma (previously aripiprazole pharmathen), Aripiprex, NSC-759266, OPC-14597, OPC-31) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 7.59 | pKi | 26 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay | B | 6.77 | pIC50 | 170 | 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 | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980] |
ChEMBL | Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay | F | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2018) 145: 74-85 [PMID:29324345] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
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 | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
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 |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method | B | 7.42 | pKi | 37.9 | nM | Ki | Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 5.94 | pKi | 1148.15 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 5.94 | pKi | 1146 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied. | B | 6.05 | pKi | 895 | nM | Ki | US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015) |
ChEMBL | Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
ChEMBL | Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (2017) 60: 4693-4713 [PMID:28489379] |
ChEMBL | Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes | B | 6.51 | pKi | 310 | nM | Ki | Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802] |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 5.71 | pKi | 1960 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
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) | B | 8.01 | pKi | 9.7 | nM | Ki | Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900] |
ChEMBL | Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied. | B | 8.1 | pKi | 8 | nM | Ki | US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015) |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | B | 8.35 | pKi | 4.5 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
ChEMBL | Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5666-5669 [PMID:20801650] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in CHO cells after 1.5 hrs by microbeta counting method | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2012) 55: 7141-7153 [PMID:22845053] |
ChEMBL | Displacement of [3H]methylspiperone from human D2 receptor by radio ligand binding assay | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945] |
ChEMBL | Displacement of [3H]-N-methylspiperone from human D2 receptor incubated for 1 hr by liquid scintillation counting method | B | 8.48 | pKi | 3.3 | nM | Ki | Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2 receptor expressed in cell membranes after 1 hr by liquid scintillation counting | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor incubated for 1 hr by liquid scintillation counting method | B | 8.48 | pKi | 3.3 | nM | Ki | Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388] |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898] |
ChEMBL | Displacement of [125I]ABN from human recombinant D2L receptor expressed in HEK cells after 60 mins by gamma counter | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem (2011) 19: 3502-3511 [PMID:21536445] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.67 | pKi | 2.13 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Binding affinity to dopamine D2 | B | 8.74 | pKi | 1.82 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cells | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2621-2625 [PMID:21353774] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 8.8 | pKi | 1.6 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay | B | 9 | pKi | <1 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in HEK293 after 1 hr | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2013) 60: 42-50 [PMID:23279866] |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
GtoPdb | - | - | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2013) 60: 42-50 [PMID:23279866] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2021) 64: 15313-15333 [PMID:34636551] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
ChEMBL |