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Assay Detail

CHEMBL879867

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

Binding
In vitro binding affinity towards Dopamine receptor D2 in rat striatum was determined using [3H]-spiperone as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
Peglion JL, Canton H, Bervoets K, Audinot V, Brocco M, Gobert A, Le Marouille-Girardon S, Millan MJ.
J Med Chem (1995) 38 : 4044 -4055
PubMed 7562940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.06 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 7.76
CHEMBL131011 1 7.38
CHEMBL130276 1 7.31
CHEMBL49247 1 6.46
CHEMBL38288 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 17.38 nM 7.76
CHEMBL131011 Ki = 41.69 nM 7.38
CHEMBL130276 Ki = 48.98 nM 7.31
CHEMBL49247 Ki = 346.74 nM 6.46
CHEMBL38288 Ki = 389.05 nM 6.41