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Assay Detail

CHEMBL674835

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

Binding
Binding affinity determined by measuring displacement of [3H]spiperone from cloned Human Dopamine receptor D3 in CHO-K1 cells
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aminopyrimidines with high affinity for both serotonin and dopamine receptors.
Wustrow D, Belliotti T, Glase S, Kesten SR, Johnson D, Colbry N, Rubin R, Blackburn A, Akunne H, Corbin A, Davis MD, Georgic L, Whetzel S, Zoski K, Heffner T, Pugsley T, Wise L.
J Med Chem (1998) 41 : 760 -771
PubMed 9513604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.58 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349426 1 10.70
CHEMBL309623 1 9.85
CHEMBL78791 1 9.10
CHEMBL164604 1 8.43
CHEMBL164723 1 8.33
CHEMBL350352 1 8.30
CHEMBL164792 1 7.96
CHEMBL165679 1 7.86
CHEMBL165047 1 7.62
CHEMBL355371 1 7.58
CHEMBL3084971 1 7.54
CHEMBL351617 1 7.50
CHEMBL165056 1 7.50
CHEMBL165440 1 7.40
CHEMBL349034 1 7.32
CHEMBL165140 1 7.27
CHEMBL165664 1 7.05
CHEMBL165689 1 6.68
CHEMBL2110308 2 6.26
CHEMBL349980 1 6.23
CHEMBL165381 1 6.10
CHEMBL166151 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349426 Ki = 0.02 nM 10.70
CHEMBL309623 Ki = 0.14 nM 9.85
CHEMBL78791 Ki = 0.8 nM 9.10
CHEMBL164604 Ki = 3.7 nM 8.43
CHEMBL164723 Ki = 4.7 nM 8.33
CHEMBL350352 Ki = 5.0 nM 8.30
CHEMBL164792 Ki = 11.0 nM 7.96
CHEMBL165679 Ki = 13.7 nM 7.86
CHEMBL165047 Ki = 24.0 nM 7.62
CHEMBL355371 Ki = 26.0 nM 7.58
CHEMBL3084971 Ki = 29.0 nM 7.54
CHEMBL351617 Ki = 32.0 nM 7.50
CHEMBL165056 Ki = 32.0 nM 7.50
CHEMBL165440 Ki = 40.0 nM 7.40
CHEMBL349034 Ki = 48.0 nM 7.32
CHEMBL165140 Ki = 54.0 nM 7.27
CHEMBL165664 Ki = 89.0 nM 7.05
CHEMBL165689 Ki = 210.0 nM 6.68
CHEMBL2110308 Ki = 550.0 nM 6.26
CHEMBL349980 Ki = 590.0 nM 6.23
CHEMBL2110308 Ki = 610.0 nM 6.21
CHEMBL165381 Ki = 800.0 nM 6.10
CHEMBL166151 Ki = 2300.0 nM 5.64