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Assay Detail

CHEMBL693825

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

Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
Abou-Gharbia M, Moyer JA, Nielsen ST, Webb M, Patel U.
J Med Chem (1995) 38 : 4026 -4032
PubMed 7562938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.10 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338611 1 7.36
CHEMBL305660 EBASTINE 4.0 1 7.35
CHEMBL17157 TERFENADINE 4.0 1 7.03
CHEMBL553331 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338611 IC50 = 44.0 nM 7.36
CHEMBL305660 EBASTINE IC50 = 45.0 nM 7.35
CHEMBL17157 TERFENADINE IC50 = 94.0 nM 7.03
CHEMBL553331 IC50 = 220.0 nM 6.66