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Assay Detail

CHEMBL2415528

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

Binding
Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
Pompeu TE, Alves FR, Figueiredo CD, Antonio CB, Herzfeldt V, Moura BC, Rates SM, Barreiro EJ, Fraga CA, Noël F.
Eur J Med Chem (2013) 66 : 122 -134
PubMed 23792350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.31 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 6.85
CHEMBL2414357 1 6.60
CHEMBL597601 1 6.41
CHEMBL2414358 1 6.31
CHEMBL2414356 1 6.17
CHEMBL2414355 1 6.10
CHEMBL2414354 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 140.0 nM 6.85
CHEMBL2414357 Ki = 250.0 nM 6.60
CHEMBL597601 Ki = 390.0 nM 6.41
CHEMBL2414358 Ki = 490.0 nM 6.31
CHEMBL2414356 Ki = 680.0 nM 6.17
CHEMBL2414355 Ki = 790.0 nM 6.10
CHEMBL2414354 Ki = 1900.0 nM 5.72