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Assay Detail

CHEMBL675089

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

Binding
In vitro inhibition of [3H]N-0437 binding to Dopamine receptor D2 in rat striatal membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model.
Liljefors T, Bøgesø KP, Hyttel J, Wikström H, Svensson K, Carlsson A.
J Med Chem (1990) 33 : 1015 -1022
PubMed 1968512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.95 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7806 1 9.21
CHEMBL7850 1 7.35
CHEMBL7549 PRECLAMOL 2.0 1 7.26
CHEMBL268240 1 7.12
CHEMBL7393 1 7.01
CHEMBL8074 1 6.77
CHEMBL7449 1 6.50
CHEMBL7381 1 6.24
CHEMBL2051756 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7806 IC50 = 0.62 nM 9.21
CHEMBL7850 IC50 = 45.0 nM 7.35
CHEMBL7549 PRECLAMOL IC50 = 55.0 nM 7.26
CHEMBL268240 IC50 = 75.0 nM 7.12
CHEMBL7393 IC50 = 98.0 nM 7.01
CHEMBL8074 IC50 = 170.0 nM 6.77
CHEMBL7449 IC50 = 320.0 nM 6.50
CHEMBL7381 IC50 = 580.0 nM 6.24
CHEMBL2051756 IC50 = 7900.0 nM 5.10