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Assay Detail

CHEMBL3614293

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

Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
8
Total Activities
8
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 Autocuration

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.
Möller D, Salama I, Kling RC, Hübner H, Gmeiner P.
Bioorg Med Chem (2015) 23 : 6195 -6209
PubMed 26299826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.74 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613873 1 7.43
CHEMBL3613879 1 7.38
CHEMBL3613880 1 7.12
CHEMBL3613877 1 7.01
CHEMBL3613874 1 6.89
CHEMBL3613878 1 6.75
CHEMBL3613875 1 5.85
CHEMBL3613876 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613873 Ki = 37.0 nM 7.43
CHEMBL3613879 Ki = 42.0 nM 7.38
CHEMBL3613880 Ki = 76.0 nM 7.12
CHEMBL3613877 Ki = 98.0 nM 7.01
CHEMBL3613874 Ki = 130.0 nM 6.89
CHEMBL3613878 Ki = 180.0 nM 6.75
CHEMBL3613875 Ki = 1400.0 nM 5.85
CHEMBL3613876 Ki = 3000.0 nM 5.52