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Assay Detail

CHEMBL669163

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

Binding
Binding affinity towards human cloned dopamine (hD3) receptor expressed in CHO cells using [3H]spiperone as radioligand
16
Total Activities
16
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(3) dopamine receptor (CHEMBL234)
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 16 7.82 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300571 1 8.96
CHEMBL64553 1 8.62
CHEMBL64508 1 7.96
CHEMBL99913 1 7.96
CHEMBL102490 1 7.56
CHEMBL88365 1 7.54
CHEMBL99849 1 7.37
CHEMBL101285 1 6.55
CHEMBL101910 1 -
CHEMBL100461 1 -
CHEMBL103900 1 -
CHEMBL100952 1 -
CHEMBL103951 1 -
CHEMBL323118 1 -
CHEMBL101032 1 -
CHEMBL319816 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300571 Ki = 1.1 nM 8.96
CHEMBL64553 Ki = 2.4 nM 8.62
CHEMBL64508 Ki = 11.0 nM 7.96
CHEMBL99913 Ki = 11.0 nM 7.96
CHEMBL102490 Ki = 27.8 nM 7.56
CHEMBL88365 Ki = 28.9 nM 7.54
CHEMBL99849 Ki = 42.5 nM 7.37
CHEMBL101285 Ki = 281.5 nM 6.55
CHEMBL101910 Ki > 400.0 nM -
CHEMBL100461 Ki > 5000.0 nM -
CHEMBL103900 Ki > 400.0 nM -
CHEMBL100952 Ki > 400.0 nM -
CHEMBL103951 Ki > 400.0 nM -
CHEMBL323118 Ki > 5000.0 nM -
CHEMBL101032 Ki > 400.0 nM -
CHEMBL319816 Ki > 1000.0 nM -