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Assay Detail

CHEMBL693832

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

Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antiallergy activity of 4-(diarylhydroxymethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
Walsh DA, Franzyshen SK, Yanni JM.
J Med Chem (1989) 32 : 105 -118
PubMed 2562852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.05 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17436 1 8.10
CHEMBL17390 1 7.38
CHEMBL17237 1 7.20
CHEMBL17157 TERFENADINE 4.0 1 6.53
CHEMBL555593 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17436 IC50 = 8.0 nM 8.10
CHEMBL17390 IC50 = 42.0 nM 7.38
CHEMBL17237 IC50 = 63.0 nM 7.20
CHEMBL17157 TERFENADINE IC50 = 295.0 nM 6.53
CHEMBL555593 IC50 = 956.0 nM 6.02