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Assay Detail

CHEMBL672379

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

Binding
Affinity of compound for Dopamine receptor D2 in rat striatal membrane determined for antagonist state (low affinity state, D2 Low) with [3H]spiperone (using ketanserin to exclude 5-HT2 receptor binding) in the presence of GTP and sodium
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

New generation dopaminergic agents. Part 8: heterocyclic bioisosteres that exploit the 7-OH-2-(aminomethyl)chroman D(2) template.
Mewshaw RE, Zhao R, Shi X, Marquis K, Brennan JA, Mazandarani H, Coupet J, Andree TH.
Bioorg Med Chem Lett (2002) 12 : 271 -274
PubMed 11814775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.86 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64553 1 8.48
CHEMBL420986 1 8.32
CHEMBL303556 1 8.23
CHEMBL93779 1 8.15
CHEMBL60185 1 7.45
CHEMBL313851 1 7.19
CHEMBL93753 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64553 Ki = 3.3 nM 8.48
CHEMBL420986 Ki = 4.81 nM 8.32
CHEMBL303556 Ki = 5.9 nM 8.23
CHEMBL93779 Ki = 7.01 nM 8.15
CHEMBL60185 Ki = 35.9 nM 7.45
CHEMBL313851 Ki = 65.1 nM 7.19
CHEMBL93753 Ki = 67.5 nM 7.17