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Assay Detail

CHEMBL840158

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

Binding
In vitro binding affinity against recombinant human dopamine receptor D2L in human liver microsomes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.
Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y.
Bioorg Med Chem Lett (2005) 15 : 1055 -1059
PubMed 15686911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.42 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178803 BLONANSERIN 4.0 1 9.85
CHEMBL360457 1 8.44
CHEMBL181469 1 8.21
CHEMBL179649 1 7.92
CHEMBL362285 1 7.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178803 BLONANSERIN Ki = 0.14 nM 9.85
CHEMBL360457 Ki = 3.6 nM 8.44
CHEMBL181469 Ki = 6.2 nM 8.21
CHEMBL179649 Ki = 11.9 nM 7.92
CHEMBL362285 Ki = 21.2 nM 7.67