aripiprazole [Ligand Id: 34] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1112 (Abilify mycite kit, Abilify maintena kit, OPC-31, Aripiprazole, OPC-14597, Abilify, Abilify Maintena)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • 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 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]
  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 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 in Rat [GtoPdb: 12] [UniProtKB: P32305]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay B 7 pKi 100 nM Ki MedChemComm (2012) 3: 580-583
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.59 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
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 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 HEK293 cells by competitive binding assay B 6.51 pKi 310 nM Ki J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
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]
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 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]-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]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 [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 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]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 Displacement of [3H]spiperone from human Dopamine D2L receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis B 9.28 pKi 0.53 nM Ki J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Displacement of [3H]spiperone from human D2LR expressed in CHO cell membranes B 9.28 pKi 0.52 nM Ki Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL Displacement of [3H]spiperone from human D2LR expressed in CHO cell membranes by radioligand binding assay B 9.28 pKi 0.52 nM Ki J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cell membranes by radioligand competition binding assay B 9.32 pKi 0.48 nM Ki Bioorg. Med. Chem. (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis B 9.32 pKi 0.48 nM Ki J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Displacement of [3H]spiperone from human Dopamine D2S receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis B 9.35 pKi 0.45 nM Ki J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Displacement of [3H]spiperone from human D2SR expressed in CHO cell membranes by radioligand binding assay B 9.42 pKi 0.38 nM Ki J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Displacement of [3H]spiperone from human D2SR expressed in CHO cell membranes B 9.42 pKi 0.38 nM Ki Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells B 9.46 pKi 0.34 nM Ki J. Med. Chem. (2015) 58: 5361-5380 [PMID:25826710]
ChEMBL Displacement of [3H]raclopride from human D2 dopamine receptor expressed in CHO cell membranes B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 543-547 [PMID:23237836]
ChEMBL Antagonistic activity at human dopamine D2 receptor measured after 60 mins by Lance Ultra cAMP assay F 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL Antagonistic activity at human dopamine D2 receptor measured after 60 mins by Ultra Lance cAMP assay B 7.76 pIC50 17.2 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay B 7.95 pIC50 11.22 nM IC50 J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay F 8.12 pIC50 7.6 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 543-547 [PMID:23237836]