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Assay Detail

CHEMBL5145666

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

Binding
Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists.
Tolentino KT, Mashinson V, Vadukoot AK, Hopkins CR.
Bioorg Med Chem Lett (2022) 61 : 128615 -128615
PubMed 35151866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.85 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5171772 1 6.25
CHEMBL5179459 1 6.05
CHEMBL5175548 1 6.04
CHEMBL5182602 1 6.02
CHEMBL5170670 1 6.01
CHEMBL5193214 1 5.67
CHEMBL5199815 1 5.63
CHEMBL5204764 1 5.61
CHEMBL5170381 1 5.39
CHEMBL5196322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5171772 Ki = 557.4 nM 6.25
CHEMBL5179459 Ki = 896.2 nM 6.05
CHEMBL5175548 Ki = 922.8 nM 6.04
CHEMBL5182602 Ki = 948.4 nM 6.02
CHEMBL5170670 Ki = 965.4 nM 6.01
CHEMBL5193214 Ki = 2119.3 nM 5.67
CHEMBL5199815 Ki = 2358.9 nM 5.63
CHEMBL5204764 Ki = 2463.8 nM 5.61
CHEMBL5170381 Ki = 4079.4 nM 5.39
CHEMBL5196322 Ki > 10000.0 nM -