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

CHEMBL958183

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

Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.
Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R.
J Med Chem (2008) 51 : 7855 -7865
PubMed 19053770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.36 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452847 1 7.70
CHEMBL454890 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452847 Ki = 19.95 nM 7.70
CHEMBL454890 Ki = 97.72 nM 7.01