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Assay Detail

CHEMBL674832

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Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D3 in CHO cell membranes
12
Total Activities
12
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 Expert

Target

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

Publication

New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Mewshaw RE, Nelson JA, Shah US, Shi X, Mazandarani H, Coupet J, Marquis K, Brennan JA, Andree TH.
Bioorg Med Chem Lett (1999) 9 : 2593 -2598
PubMed 10498215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.99 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87192 1 8.94
CHEMBL327782 1 8.70
CHEMBL59752 1 8.55
CHEMBL314174 1 8.39
CHEMBL329398 1 8.13
CHEMBL87137 1 8.06
CHEMBL64508 1 7.96
CHEMBL89037 1 7.91
CHEMBL64283 1 7.71
CHEMBL86504 1 7.38
CHEMBL89420 1 7.17
CHEMBL87067 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87192 Ki = 1.15 nM 8.94
CHEMBL327782 Ki = 2.0 nM 8.70
CHEMBL59752 Ki = 2.8 nM 8.55
CHEMBL314174 Ki = 4.1 nM 8.39
CHEMBL329398 Ki = 7.4 nM 8.13
CHEMBL87137 Ki = 8.8 nM 8.06
CHEMBL64508 Ki = 11.0 nM 7.96
CHEMBL89037 Ki = 12.2 nM 7.91
CHEMBL64283 Ki = 19.5 nM 7.71
CHEMBL86504 Ki = 41.8 nM 7.38
CHEMBL89420 Ki = 67.2 nM 7.17
CHEMBL87067 Ki = 94.6 nM 7.02