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Assay Detail

CHEMBL5738136

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding Assay: 225 nL of the solutions of the non-specific ligand or the compounds of the present invention at each concentration (in case of vehicle, final concentration 0.3% DMSO) were added in each well of a 384-well white/clear bottom microplate (3706, Corning). Jump-In HEK Cell membranes (final reaction amount: 4 μg/well), SPA beads (final reaction amount: 0.2 mg/well) and Tris-HCl buffer were mixed and the mixed solution was left still for more than 60 min at 4° C. Then, 50 μL of the mixture was added to each well of the plate. In addition, 25 μL of 6 nM [3H]-Metylspiperone (final concentration: 2 nM) was added to each well. The plate was sealed by putting TopSeal-A 96/384 well (6050185, PerkinElmer) on the top of the plate, mixed using stirring deaerator (Welltornado, FK-62, Sakaki) and incubated for 120 min at 25° C. After incubation, the radioactivity of [3H]-Metylspiperone which was binded to D3 receptor was determined by liquid scintillation counter (1450 Microbeta, PerkinElmer) in each well. Non-specific binding was calculated based on the radioactivity of [3II]-Metylspiperone in the presence of 10 μM non-labeled Butaclamol. The total binding was calculated based on the radioactivity of [3H]-Metylspiperone in the absence of the compounds of the present invention (Vehicle). The Ki values were calculated from dose-response curves.
ChEMBL ↗
417
Total Activities
137
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nitrogen-containing condensed ring compounds having dopamine D3 antagonistic effect
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 139 6.31 7.36
kon 139 - -
k_off 139 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5958714 — — 3 7.36
CHEMBL5990865 — — 3 7.10
CHEMBL6004699 — — 3 6.92
CHEMBL5841759 — — 3 6.85
CHEMBL5823796 — — 3 6.85
CHEMBL6029030 — — 3 6.85
CHEMBL5801091 — — 3 6.82
CHEMBL5866064 — — 3 6.77
CHEMBL5898773 — — 3 6.77
CHEMBL5804436 — — 3 6.72
CHEMBL5948904 — — 3 6.68
CHEMBL5821968 — — 3 6.66
CHEMBL5747557 — — 3 6.64
CHEMBL5787369 — — 3 6.64
CHEMBL5745240 — — 3 6.62
CHEMBL5926122 — — 6 6.58
CHEMBL5810433 — — 3 6.55
CHEMBL5769559 — — 3 6.54
CHEMBL5921899 — — 3 6.54
CHEMBL5979572 — — 3 6.54
CHEMBL5825746 — — 3 6.51
CHEMBL5926812 — — 3 6.51
CHEMBL5854979 — — 3 6.48
CHEMBL5783780 — — 3 6.48
CHEMBL5843487 — — 3 6.48
CHEMBL5925320 — — 3 6.47
CHEMBL6034513 — — 3 6.46
CHEMBL6011163 — — 3 6.43
CHEMBL5770832 — — 3 6.43
CHEMBL6023248 — — 3 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5958714 — Ki = 44.0 nM 7.36
CHEMBL5990865 — Ki = 79.0 nM 7.10
CHEMBL6004699 — Ki = 120.0 nM 6.92
CHEMBL5841759 — Ki = 140.0 nM 6.85
CHEMBL6029030 — Ki = 140.0 nM 6.85
CHEMBL5823796 — Ki = 140.0 nM 6.85
CHEMBL5801091 — Ki = 150.0 nM 6.82
CHEMBL5866064 — Ki = 170.0 nM 6.77
CHEMBL5898773 — Ki = 170.0 nM 6.77
CHEMBL5804436 — Ki = 190.0 nM 6.72
CHEMBL5948904 — Ki = 210.0 nM 6.68
CHEMBL5821968 — Ki = 220.0 nM 6.66
CHEMBL5747557 — Ki = 230.0 nM 6.64
CHEMBL5787369 — Ki = 230.0 nM 6.64
CHEMBL5745240 — Ki = 240.0 nM 6.62
CHEMBL5926122 — Ki = 260.0 nM 6.58
CHEMBL5926122 — Ki = 280.0 nM 6.55
CHEMBL5810433 — Ki = 280.0 nM 6.55
CHEMBL5921899 — Ki = 290.0 nM 6.54
CHEMBL5979572 — Ki = 290.0 nM 6.54
CHEMBL5769559 — Ki = 290.0 nM 6.54
CHEMBL5926812 — Ki = 310.0 nM 6.51
CHEMBL5825746 — Ki = 310.0 nM 6.51
CHEMBL5843487 — Ki = 330.0 nM 6.48
CHEMBL5783780 — Ki = 330.0 nM 6.48
CHEMBL5854979 — Ki = 330.0 nM 6.48
CHEMBL5925320 — Ki = 340.0 nM 6.47
CHEMBL6034513 — Ki = 350.0 nM 6.46
CHEMBL6011163 — Ki = 370.0 nM 6.43
CHEMBL5770832 — Ki = 370.0 nM 6.43
CHEMBL5902278 — Ki = 380.0 nM 6.42
CHEMBL6023248 — Ki = 380.0 nM 6.42
CHEMBL5891513 — Ki = 400.0 nM 6.40
CHEMBL5983794 — Ki = 400.0 nM 6.40
CHEMBL6008861 — Ki = 410.0 nM 6.39
CHEMBL5814275 — Ki = 430.0 nM 6.37
CHEMBL5972372 — Ki = 460.0 nM 6.34
CHEMBL6027608 — Ki = 460.0 nM 6.34
CHEMBL5852484 — Ki = 480.0 nM 6.32
CHEMBL5904674 — Ki = 480.0 nM 6.32
CHEMBL6044734 — Ki = 490.0 nM 6.31
CHEMBL5823486 — Ki = 500.0 nM 6.30
CHEMBL5828803 — Ki = 500.0 nM 6.30
CHEMBL5880657 — Ki = 500.0 nM 6.30
CHEMBL5817877 — Ki = 510.0 nM 6.29
CHEMBL5882421 — Ki = 520.0 nM 6.28
CHEMBL5821204 — Ki = 530.0 nM 6.28
CHEMBL5876040 — Ki = 520.0 nM 6.28
CHEMBL5886490 — Ki = 540.0 nM 6.27
CHEMBL5816980 — Ki = 550.0 nM 6.26