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Assay Detail

CHEMBL673355

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

Binding
Binding affinity towards dopamine receptor D2 in rat striatal membrane using [3H]spiperone
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.
Caprathe BW, Jaen JC, Wise LD, Heffner TG, Pugsley TA, Meltzer LT, Parvez M.
J Med Chem (1991) 34 : 2736 -2746
PubMed 1680195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.71 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93428 1 6.24
CHEMBL150550 2 6.07
CHEMBL93972 1 5.95
CHEMBL328548 1 5.91
CHEMBL91453 1 5.66
CHEMBL276500 1 5.64
CHEMBL329444 1 5.46
CHEMBL92784 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93428 IC50 = 574.0 nM 6.24
CHEMBL150550 IC50 = 860.0 nM 6.07
CHEMBL93972 IC50 = 1129.0 nM 5.95
CHEMBL328548 IC50 = 1235.0 nM 5.91
CHEMBL91453 IC50 = 2197.0 nM 5.66
CHEMBL150550 IC50 = 2243.0 nM 5.65
CHEMBL276500 IC50 = 2280.0 nM 5.64
CHEMBL329444 IC50 = 3428.0 nM 5.46
CHEMBL92784 IC50 = 15550.0 nM 4.81