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Assay Detail

CHEMBL5250277

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

Binding
Displacement of [3H]N-methylspiperone from D3 receptor in HEK293 cell membrane assessed as inhibition constant
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.
Tolentino KT, Mashinson V, Sharma MK, Chhonker YS, Murry DJ, Hopkins CR.
Eur J Med Chem (2022) 244 : 114840 -114840
PubMed 36283180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.16 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5274285 1 6.93
CHEMBL5289958 1 6.46
CHEMBL5272689 1 6.42
CHEMBL5288298 1 6.29
CHEMBL5182602 1 6.02
CHEMBL5204764 1 5.61
CHEMBL5170381 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5274285 Ki = 118.0 nM 6.93
CHEMBL5289958 Ki = 345.0 nM 6.46
CHEMBL5272689 Ki = 376.0 nM 6.42
CHEMBL5288298 Ki = 512.0 nM 6.29
CHEMBL5182602 Ki = 948.0 nM 6.02
CHEMBL5204764 Ki = 2463.0 nM 5.61
CHEMBL5170381 Ki = 4079.0 nM 5.39