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Assay Detail

CHEMBL670410

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Functional
Agonistic activity towards dopamine D2 receptor using radioligand [3H]quinpirole in rat striatal membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8.01 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64553 1 9.80
CHEMBL300571 1 9.46
CHEMBL99913 1 8.80
CHEMBL102490 1 8.59
CHEMBL64508 1 8.44
CHEMBL99849 1 8.36
CHEMBL88365 1 8.26
CHEMBL323118 1 8.10
CHEMBL101285 1 8.02
CHEMBL101032 1 7.79
CHEMBL101910 1 7.71
CHEMBL100952 1 7.19
CHEMBL103951 1 7.17
CHEMBL100461 1 6.95
CHEMBL103900 1 6.92
CHEMBL319816 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64553 Ki = 0.16 nM 9.80
CHEMBL300571 Ki = 0.35 nM 9.46
CHEMBL99913 Ki = 1.6 nM 8.80
CHEMBL102490 Ki = 2.6 nM 8.59
CHEMBL64508 Ki = 3.6 nM 8.44
CHEMBL99849 Ki = 4.4 nM 8.36
CHEMBL88365 Ki = 5.5 nM 8.26
CHEMBL323118 Ki = 7.9 nM 8.10
CHEMBL101285 Ki = 9.6 nM 8.02
CHEMBL101032 Ki = 16.2 nM 7.79
CHEMBL101910 Ki = 19.7 nM 7.71
CHEMBL100952 Ki = 64.7 nM 7.19
CHEMBL103951 Ki = 68.4 nM 7.17
CHEMBL100461 Ki = 113.0 nM 6.95
CHEMBL103900 Ki = 120.0 nM 6.92
CHEMBL319816 Ki = 237.0 nM 6.62