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Assay Detail

CHEMBL671247

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

Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.
Mewshaw RE, Husbands M, Gildersleeve ES, Webb MB, Shi X, Mazandarani H, Cockett MI, Ochalski R, Brennan JA, Abou-Gharbia M, Marquis K, McGaughey GB, Coupet J, Andree TH.
Bioorg Med Chem Lett (1998) 8 : 295 -300
PubMed 9871673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.85 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319816 1 7.57
CHEMBL64508 1 7.09
CHEMBL103951 1 7.03
CHEMBL102490 1 6.86
CHEMBL100461 1 6.56
CHEMBL101285 1 6.53
CHEMBL99849 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319816 Ki = 27.2 nM 7.57
CHEMBL64508 Ki = 80.6 nM 7.09
CHEMBL103951 Ki = 94.0 nM 7.03
CHEMBL102490 Ki = 137.0 nM 6.86
CHEMBL100461 Ki = 277.0 nM 6.56
CHEMBL101285 Ki = 297.0 nM 6.53
CHEMBL99849 Ki = 500.0 nM 6.30