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Assay Detail

CHEMBL673445

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

Binding
Binding affinity against human Dopamine receptor D3 in CHO-K1 cells using [3H]spiperone as radioligand
5
Total Activities
5
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 Autocuration

Target

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

Publication

Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.
Glase SA, Akunne HC, Heffner TG, Jaen JC, MacKenzie RG, Meltzer LT, Pugsley TA, Smith SJ, Wise LD.
J Med Chem (1996) 39 : 3179 -3187
PubMed 8759640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.41 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431367 ROXINDOLE 2.0 1 9.40
CHEMBL109101 1 8.59
CHEMBL110489 1 8.19
CHEMBL109063 1 8.15
CHEMBL108463 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431367 ROXINDOLE Ki = 0.4 nM 9.40
CHEMBL109101 Ki = 2.6 nM 8.59
CHEMBL110489 Ki = 6.5 nM 8.19
CHEMBL109063 Ki = 7.0 nM 8.15
CHEMBL108463 Ki = 20.0 nM 7.70