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Assay Detail

CHEMBL4045108

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ADMET
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
Xiamuxi H, Wang Z, Li J, Wang Y, Wu C, Yang F, Jiang X, Liu Y, Zhao Q, Chen W, Zhang J, Xie Y, Hu T, Xu M, Guo S, Akber Aisa H, He Y, Shen J.
Bioorg Med Chem (2017) 25 : 4904 -4916
PubMed 28774576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.76 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104261 1 6.91
CHEMBL4083333 1 6.90
CHEMBL4094825 1 6.88
CHEMBL4087132 1 6.79
CHEMBL4102670 1 6.75
CHEMBL85 RISPERIDONE 4.0 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104261 IC50 = 123.0 nM 6.91
CHEMBL4083333 IC50 = 127.0 nM 6.90
CHEMBL4094825 IC50 = 132.0 nM 6.88
CHEMBL4087132 IC50 = 162.0 nM 6.79
CHEMBL4102670 IC50 = 177.0 nM 6.75
CHEMBL85 RISPERIDONE IC50 = 454.0 nM 6.34