Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4709845

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

ADMET
Displacement of [3H]pyrilamine from guinea pig cerebellum histamine H1 receptor measured after 60 mins by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Isoquinolinone derivatives as potent CNS multi-receptor D/5-HT/5-HT/5-HT/5-HT agents: Synthesis and pharmacological evaluation.
Jin J,Zhang K,Dou F,Hao C,Zhang Y,Cao X,Gao L,Xiong J,Liu X,Liu BF,Zhang G,Chen Y
Eur J Med Chem (2020) 207 : 112709 -112709
PubMed 32877805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.91 7.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 7.49
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.31
CHEMBL4743324 1 6.93
CHEMBL4764679 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 32.6 nM 7.49
CHEMBL1112 ARIPIPRAZOLE Ki = 48.9 nM 7.31
CHEMBL4743324 Ki = 117.9 nM 6.93
CHEMBL4764679 Ki = 1196.0 nM 5.92