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Assay Detail

CHEMBL3875680

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

ADMET
Displacement of [3H]prazosin from adrenergic alpha1 receptor in Sprague-Dawley rat cerebral cortex 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 Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 6.69 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 7.24
CHEMBL3885471 1 6.93
CHEMBL3884161 1 6.83
CHEMBL3884325 1 6.47
CHEMBL3883955 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 57.8 nM 7.24
CHEMBL3885471 Ki = 118.0 nM 6.93
CHEMBL3884161 Ki = 147.0 nM 6.83
CHEMBL3884325 Ki = 337.0 nM 6.47
CHEMBL3883955 Ki = 1098.0 nM 5.96