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Assay Detail

CHEMBL3875679

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

ADMET
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum incubated for 60 mins by liquid scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
Cao X, Chen Y, Zhang Y, Qiu Y, Yu M, Xu X, Liu X, Liu BF, Zhang G.
Eur J Med Chem (2016) 124 : 713 -728
PubMed 27639363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.90 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3885471 1 7.78
CHEMBL85 RISPERIDONE 4.0 1 7.37
CHEMBL3884325 1 6.94
CHEMBL3884161 1 6.73
CHEMBL3883955 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3885471 Ki = 16.6 nM 7.78
CHEMBL85 RISPERIDONE Ki = 42.6 nM 7.37
CHEMBL3884325 Ki = 115.0 nM 6.94
CHEMBL3884161 Ki = 186.0 nM 6.73
CHEMBL3883955 Ki = 1998.0 nM 5.70