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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
1 CHEMBL1112_lig_chart_1 Alpha-1a adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • This target only has 1 pki data point
2 CHEMBL1112_lig_chart_2 Alpha-1b adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • This target only has 1 pki data point
3 CHEMBL1112_lig_chart_3 Alpha-2a adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • This target only has 1 pki data point
4 CHEMBL1112_lig_chart_4 Alpha-2b adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
  • This target only has 1 pki data point
5 CHEMBL1112_lig_chart_5 Alpha-2c adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
6 CHEMBL1112_lig_chart_6 Dopamine D1 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
7 CHEMBL1112_lig_chart_7 Dopamine D2 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
8 CHEMBL1112_lig_chart_8 Dopamine D3 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
9 CHEMBL1112_lig_chart_9 Dopamine D4 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
10 CHEMBL1112_lig_chart_10 Dopamine D5 receptor Human
There should be some charts here, you may need to enable JavaScript!
11 CHEMBL1112_lig_chart_11 HERG Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
12 CHEMBL1112_lig_chart_12 Histamine H1 receptor HumanRatGuinea pig
There should be some charts here, you may need to enable JavaScript!
  • Histone H1.0 in Human [ChEMBL: CHEMBL3707465] [UniProtKB: P07305]
  • This target only has 1 pki data point
13 CHEMBL1112_lig_chart_13 Histone H1.0 Human
There should be some charts here, you may need to enable JavaScript!
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • This target only has 1 pki data point
14 CHEMBL1112_lig_chart_14 Muscarinic acetylcholine receptor M1 Human
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 1 pki data point
15 CHEMBL1112_lig_chart_15 Muscarinic acetylcholine receptor M2 Human
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
16 CHEMBL1112_lig_chart_16 Muscarinic acetylcholine receptor M3 Human
There should be some charts here, you may need to enable JavaScript!
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
17 CHEMBL1112_lig_chart_17 Muscarinic acetylcholine receptor M4 Human
There should be some charts here, you may need to enable JavaScript!
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 1 pki data point
18 CHEMBL1112_lig_chart_18 Muscarinic acetylcholine receptor M5 Human
There should be some charts here, you may need to enable JavaScript!
  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 0 pki data point
19 CHEMBL1112_lig_chart_19 P-glycoprotein 1 Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
20 CHEMBL1112_lig_chart_20 Serotonin 1a (5-HT1a) receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
21 CHEMBL1112_lig_chart_21 Serotonin 1b (5-HT1b) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
22 CHEMBL1112_lig_chart_22 Serotonin 1d (5-HT1d) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
  • This target only has 1 pki data point
23 CHEMBL1112_lig_chart_23 Serotonin 1e (5-HT1e) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
24 CHEMBL1112_lig_chart_24 Serotonin 2a (5-HT2a) receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
25 CHEMBL1112_lig_chart_25 Serotonin 2b (5-HT2b) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
26 CHEMBL1112_lig_chart_26 Serotonin 2c (5-HT2c) receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
27 CHEMBL1112_lig_chart_27 Serotonin 3 (5-HT3) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • This target only has 1 pki data point
28 CHEMBL1112_lig_chart_28 Serotonin 3a (5-HT3a) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • This target only has 1 pki data point
29 CHEMBL1112_lig_chart_29 Serotonin 5a (5-HT5a) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 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]
30 CHEMBL1112_lig_chart_30 Serotonin 6 (5-HT6) receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
31 CHEMBL1112_lig_chart_31 Serotonin 7 (5-HT7) receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
32 CHEMBL1112_lig_chart_32 Serotonin transporter HumanRat
There should be some charts here, you may need to enable JavaScript!
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]