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Assay Detail

CHEMBL3744548

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

Binding
Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of amide, sulfonamide and urea benzisoxazole derivatives as potential atypical antipsychotics
Chen Y, Lan Y, Cao X, Xu X, Zhang J, Yu M, Liu X, Liu B, Zhang G
Medchemcomm (2015) 6 : 831 -838
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.56 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.55
CHEMBL3741292 1 8.06
CHEMBL3740256 1 7.49
CHEMBL3740925 1 7.07
CHEMBL3740807 1 7.06
CHEMBL42 CLOZAPINE 4.0 1 6.88
CHEMBL3742070 1 6.75
CHEMBL3742368 1 6.72
CHEMBL3741140 1 6.71
CHEMBL3742391 1 6.68
CHEMBL3739523 1 6.23
CHEMBL3740759 1 6.12
CHEMBL3740680 1 5.96
CHEMBL3740636 1 5.92
CHEMBL3741924 1 5.90
CHEMBL3741596 1 5.89
CHEMBL3739935 1 5.89
CHEMBL3742136 1 5.89
CHEMBL3740811 1 5.86
CHEMBL3741553 1 5.60
CHEMBL3739805 1 -
CHEMBL3741925 1 -
CHEMBL3742362 1 -
CHEMBL3741933 1 -
CHEMBL3741516 1 -
CHEMBL3741698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 2.8 nM 8.55
CHEMBL3741292 Ki = 8.7 nM 8.06
CHEMBL3740256 Ki = 32.6 nM 7.49
CHEMBL3740925 Ki = 85.6 nM 7.07
CHEMBL3740807 Ki = 86.8 nM 7.06
CHEMBL42 CLOZAPINE Ki = 130.7 nM 6.88
CHEMBL3742070 Ki = 178.1 nM 6.75
CHEMBL3742368 Ki = 190.4 nM 6.72
CHEMBL3741140 Ki = 194.6 nM 6.71
CHEMBL3742391 Ki = 210.9 nM 6.68
CHEMBL3739523 Ki = 589.7 nM 6.23
CHEMBL3740759 Ki = 758.8 nM 6.12
CHEMBL3740680 Ki = 1099.1 nM 5.96
CHEMBL3740636 Ki = 1191.1 nM 5.92
CHEMBL3741924 Ki = 1268.2 nM 5.90
CHEMBL3741596 Ki = 1273.8 nM 5.89
CHEMBL3739935 Ki = 1287.1 nM 5.89
CHEMBL3742136 Ki = 1290.8 nM 5.89
CHEMBL3740811 Ki = 1382.5 nM 5.86
CHEMBL3741553 Ki = 2500.0 nM 5.60
CHEMBL3739805 Ki > 10000.0 nM -
CHEMBL3741925 Ki > 10000.0 nM -
CHEMBL3742362 Ki > 10000.0 nM -
CHEMBL3741933 Ki > 10000.0 nM -
CHEMBL3741516 Ki > 10000.0 nM -
CHEMBL3741698 Ki > 10000.0 nM -