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Assay Detail

CHEMBL671370

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

Binding
Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Rowley M, Broughton HB, Collins I, Baker R, Emms F, Marwood R, Patel S, Patel S, Ragan CI, Freedman SB, Leeson PD.
J Med Chem (1996) 39 : 1943 -1945
PubMed 8642551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.02 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL42 CLOZAPINE 4.0 1 7.13
CHEMBL61195 1 6.89
CHEMBL58296 1 6.80
CHEMBL61080 1 6.62
CHEMBL61079 1 6.54
CHEMBL6416 1 6.28
CHEMBL293341 1 -
CHEMBL444309 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL42 CLOZAPINE Ki = 74.0 nM 7.13
CHEMBL61195 Ki = 130.0 nM 6.89
CHEMBL58296 Ki = 160.0 nM 6.80
CHEMBL61080 Ki = 240.0 nM 6.62
CHEMBL61079 Ki = 290.0 nM 6.54
CHEMBL6416 Ki = 520.0 nM 6.28
CHEMBL293341 Ki > 1700.0 nM -
CHEMBL444309 Ki > 1700.0 nM -