ChEMBL ligand: CHEMBL243712 (Aminosultopride, Amisulprida, Amisulpride, APD-421, APD421, Barhemsys, DAN-2163, Deniban, NSC-760085, Socian, Solian, Solian 100, Solian 200, Solian 400, Solian 50, Sulamid)
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] There should be some charts here, you may need to enable JavaScript!
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020] 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
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells	B	6.2	pKi	630.96	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-LSD from human 5-HT2B receptor assessed as inhibition constant incubated for 1.5 hrs	B	7.89	pKi	13	nM	Ki	J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	B	7.6	pKi	25.12	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay	B	7.94	pKi	11.5	nM	Ki	Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb	-	-	7.8	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells	B	7.9	pKi	12.59	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb	-	-	8	pKi	-	-	-	Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Mol Pharmacol (1993) 43: 749-54 [PMID:8099194]
ChEMBL	Displacement of [3H]N-methyl-spiperone from D2R (unknown origin) assessed as inhibition constant by competition binding assay	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
ChEMBL	Antagonist activity at DRD2 (unknown origin)	F	7.89	pIC50	12.98	nM	IC50	J Med Chem (2024) 67: 13829-13851 [PMID:39082833]
ChEMBL	Binding of Compound 102 to Dopamine D2 Receptors (Membrane Preparation): The ability of Compound 102 to bind the dopamine D2 receptor in a membrane preparation was examined. Medium was removed from dopamine D2 receptor cells and washed with PBS. A lysis buffer (250 mM sucrose, 1 nM EDTA, 10 mM Tris HCl buffered at pH 7.2 plus protease inhibitors) was added and cells scrapped using a plate scrapper. Cells were homogenized with 20 manual up and down strokes in a glass homogenizer. Intact cells, nuclei, and cell debris were removed by centrifugation of the homogenate at 500× g for 10 minutes at 4° C., the supernatant was removed, and the pellet resuspended in assay buffer. Membrane preparations were incubated with 3H spiperone until equilibration. Separation of bound from free radioligand was carried out using a Packard Filtermate Harvester and glass filter plates. Radioactivity was measured using a Packard Topcount. To 20 μL of D2 membranes were mixed 20 μL of 3H spiperone and 10 μL test compound or reference ligand in binding buffer in a nonbinding 96 well plate, and incubated for <120 minutes. Prior to filtration, a 96 well harvest filter plate was coated with 0.33% polyethyleneimine for 30 minutes and then washed with assay buffer. The binding reaction was transferred to the filter plate and washed three times with wash buffer, dried, scintillant added, and radioactivity counted on a Topcount NXT.	B	8.07	pIC50	8.5	nM	IC50	US-10167256-B2. Psychotrophic agents and uses thereof (2019)
ChEMBL	Binding of Compound 102 to Dopamine D2 Receptors (Membrane Preparation): The ability of Compound 102 to bind the dopamine D2 receptor in a membrane preparation was examined. Medium was removed from dopamine D2 receptor cells and washed with PBS. A lysis buffer (250 mM sucrose, 1 nM EDTA, 10 mM Tris HCl buffered at pH 7.2 plus protease inhibitors) was added and cells scrapped using a plate scrapper. Cells were homogenized with 20 manual up and down strokes in a glass homogenizer. Intact cells, nuclei, and cell debris were removed by centrifugation of the homogenate at 500×g for 10 minutes at 4° C., the supernatant was removed, and the pellet resuspended in assay buffer.Membrane preparations were incubated with 3H spiperone until equilibration. Separation of bound from free radioligand was carried out using a Packard Filtermate Harvester and glass filter plates. Radioactivity was measured using a Packard Topcount. To 20 μL of D2 membranes were mixed 20 μL of 3H spiperone and 10 μL test compound or reference ligand in binding buffer in a nonbinding 96 well plate, and incubated for <120 minutes. Prior to filtration, a 96 well harvest filter plate was coated with 0.33% polyethyleneimine for 30 minutes and then washed with assay buffer. The binding reaction was transferred to the filter plate and washed three times with wash buffer, dried, scintillant added, and radioactivity counted on a Topcount NXT.	B	8.07	pIC50	8.5	nM	IC50	US-10259786-B2. Psychotropic agents and uses thereof (2019)
ChEMBL	Antagonistic activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of dopamine-induced calcium flux by fluo-4 dye based FLIPR assay	F	8.52	pIC50	3.04	nM	IC50	Eur J Med Chem (2016) 123: 332-353 [PMID:27487565]
ChEMBL	Dopamine D2 Receptors (Cell-Based Assay): The ability of Compound 102 to bind dopamine D2 receptors was measured in a cell-based assay. Dopamine D2 receptor cells were seeded in a half a black, clear-bottomed 96 well plate. At a density of 15,000 cells/well to a volume of 25 μL and were left to incubate overnight. Calcium 5 dye in HEPES buffered HBSS (Hanks' balanced salt solution) was prepared and 10 μL was added to each well and the mixture was left to sit at 37° C. for 1 hour. After equilibration, 5 μL of the test compound and controls were added to the wells and incubated at room temperature for 10 minutes. Fluorescence was measured every 1.52 seconds. After 20 seconds 10 μL of dopamine (at EC80 concentration) was added and the fluorescence monitored for 2 minutes with excitation at 452 nm and emission at 525 nm.	B	8.82	pIC50	1.5	nM	IC50	US-10167256-B2. Psychotrophic agents and uses thereof (2019)
ChEMBL	Binding of Compound 102 to Dopamine D2 Receptors (Cell-Based Assay): The ability of Compound 102 to bind dopamine D2 receptors was measured in a cell-based assay. Dopamine D2 receptor cells were seeded in a half a black, clear-bottomed 96 well plate. At a density of 15,000 cells/well to a volume of 25 μL and were left to incubate overnight. Calcium 5 dye in HEPES buffered HBSS (Hanks' balanced salt solution) was prepared and 10 μL was added to each well and the mixture was left to sit at 37° C. for 1 hour. After equilibration, 5 μL of the test compound and controls were added to the wells and incubated at room temperature for 10 minutes. Fluorescence was measured every 1.52 seconds. After 20 seconds 10 μL of dopamine (at EC80 concentration) was added and the fluorescence monitored for 2 minutes with excitation at 452 nm and emission at 525 nm.	B	8.82	pIC50	1.5	nM	IC50	US-10259786-B2. Psychotropic agents and uses thereof (2019)
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	8.4	pKi	3.98	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]N-methyl-spiperone from D3R (unknown origin) assessed as inhibition constant by competition binding assay	B	8.46	pKi	3.5	nM	Ki	Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb	-	-	7.4	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]