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Assay Detail

CHEMBL4054779

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

Binding
Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior.
Stößel A, Brox R, Purkayastha N, Hübner H, Hocke C, Prante O, Gmeiner P.
Bioorg Med Chem (2017) 25 : 3491 -3499
PubMed 28495386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.76 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 1 9.57
CHEMBL4064974 1 9.51
CHEMBL4074669 1 9.51
CHEMBL4085920 1 8.92
CHEMBL4096858 1 8.62
CHEMBL142020 1 8.46
CHEMBL4060837 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE Ki = 0.27 nM 9.57
CHEMBL4064974 Ki = 0.31 nM 9.51
CHEMBL4074669 Ki = 0.31 nM 9.51
CHEMBL4085920 Ki = 1.2 nM 8.92
CHEMBL4096858 Ki = 2.4 nM 8.62
CHEMBL142020 Ki = 3.5 nM 8.46
CHEMBL4060837 Ki = 200.0 nM 6.70