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Assay Detail

CHEMBL672206

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

Binding
Binding affinity determined by measuring its ability to displace [3H]N-0437 radioligand in CHO-K1 cells on Cloned Human Dopamine receptor D2
25
Total Activities
24
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(2) dopamine receptor (CHEMBL217)
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 25 7.56 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164792 1 8.52
CHEMBL349426 1 8.49
CHEMBL78791 1 8.47
CHEMBL164604 1 8.33
CHEMBL165047 1 8.32
CHEMBL165679 1 8.28
CHEMBL165664 1 8.24
CHEMBL351617 1 8.22
CHEMBL165056 1 8.22
CHEMBL165140 1 8.13
CHEMBL349034 1 8.07
CHEMBL350352 1 7.96
CHEMBL355371 1 7.92
CHEMBL164723 1 7.60
CHEMBL3084971 1 7.55
CHEMBL309623 1 7.42
CHEMBL164979 1 7.41
CHEMBL166252 1 7.34
CHEMBL165440 1 6.96
CHEMBL2110308 2 6.80
CHEMBL165689 1 6.75
CHEMBL349980 1 6.62
CHEMBL165381 1 5.62
CHEMBL166151 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164792 Ki = 3.0 nM 8.52
CHEMBL349426 Ki = 3.2 nM 8.49
CHEMBL78791 Ki = 3.4 nM 8.47
CHEMBL164604 Ki = 4.7 nM 8.33
CHEMBL165047 Ki = 4.8 nM 8.32
CHEMBL165679 Ki = 5.2 nM 8.28
CHEMBL165664 Ki = 5.7 nM 8.24
CHEMBL351617 Ki = 6.0 nM 8.22
CHEMBL165056 Ki = 6.0 nM 8.22
CHEMBL165140 Ki = 7.4 nM 8.13
CHEMBL349034 Ki = 8.5 nM 8.07
CHEMBL350352 Ki = 11.0 nM 7.96
CHEMBL355371 Ki = 12.0 nM 7.92
CHEMBL164723 Ki = 25.0 nM 7.60
CHEMBL3084971 Ki = 28.0 nM 7.55
CHEMBL309623 Ki = 38.0 nM 7.42
CHEMBL164979 Ki = 39.0 nM 7.41
CHEMBL166252 Ki = 46.0 nM 7.34
CHEMBL165440 Ki = 110.0 nM 6.96
CHEMBL2110308 Ki = 160.0 nM 6.80
CHEMBL165689 Ki = 180.0 nM 6.75
CHEMBL349980 Ki = 240.0 nM 6.62
CHEMBL2110308 Ki = 320.0 nM 6.50
CHEMBL165381 Ki = 2400.0 nM 5.62
CHEMBL166151 Ki = 4800.0 nM 5.32