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Assay Detail

CHEMBL898620

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

Binding
Displacement of [3H]spiperone from human Dopamine D3 receptor expressed in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.
Awadallah FM, Müller F, Lehmann J, Abadi AH.
Bioorg Med Chem (2007) 15 : 5811 -5818
PubMed 17576067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.77 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240996 1 7.85
CHEMBL393492 1 7.52
CHEMBL240774 1 7.45
CHEMBL394110 1 7.18
CHEMBL395933 1 7.10
CHEMBL398813 1 6.99
CHEMBL238916 1 6.97
CHEMBL238917 1 6.73
CHEMBL394080 1 6.71
CHEMBL268371 1 6.61
CHEMBL238915 1 6.54
CHEMBL239700 1 6.51
CHEMBL238717 1 6.28
CHEMBL240995 1 6.18
CHEMBL239917 1 5.92
CHEMBL238718 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240996 Ki = 14.0 nM 7.85
CHEMBL393492 Ki = 30.0 nM 7.52
CHEMBL240774 Ki = 35.8 nM 7.45
CHEMBL394110 Ki = 66.0 nM 7.18
CHEMBL395933 Ki = 80.0 nM 7.10
CHEMBL398813 Ki = 102.0 nM 6.99
CHEMBL238916 Ki = 107.0 nM 6.97
CHEMBL238917 Ki = 187.0 nM 6.73
CHEMBL394080 Ki = 195.0 nM 6.71
CHEMBL268371 Ki = 247.0 nM 6.61
CHEMBL238915 Ki = 287.0 nM 6.54
CHEMBL239700 Ki = 306.0 nM 6.51
CHEMBL238717 Ki = 527.0 nM 6.28
CHEMBL240995 Ki = 660.0 nM 6.18
CHEMBL239917 Ki = 1204.0 nM 5.92
CHEMBL238718 Ki = 1780.0 nM 5.75