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Assay Detail

CHEMBL651364

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

Binding
Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D2
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
Jaen JC, Caprathe BW, Pugsley TA, Wise LD, Akunne H.
J Med Chem (1993) 36 : 3929 -3936
PubMed 7902870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.03 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.36
CHEMBL340211 AZAPERONE 2.0 1 7.28
CHEMBL129237 1 7.14
CHEMBL339963 1 7.00
CHEMBL129159 1 6.55
CHEMBL339033 1 6.39
CHEMBL60859 BMY-14802 1 5.47
CHEMBL129768 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.44 nM 9.36
CHEMBL340211 AZAPERONE Ki = 52.0 nM 7.28
CHEMBL129237 Ki = 73.0 nM 7.14
CHEMBL339963 Ki = 101.0 nM 7.00
CHEMBL129159 Ki = 279.0 nM 6.55
CHEMBL339033 Ki = 403.0 nM 6.39
CHEMBL60859 BMY-14802 Ki = 3346.0 nM 5.47
CHEMBL129768 Ki > 5000.0 nM -