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Assay Detail

CHEMBL5117904

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

Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
Gjervig Jensen K, Tornby Christoffersen C, Graulund Hvenegaard M, Didriksen M, Jørgensen M.
Bioorg Med Chem Lett (2022) 72 : 128879 -128879
PubMed 35809818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.29 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191141 1 8.40
CHEMBL5201983 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191141 Ki = 4.0 nM 8.40
CHEMBL5201983 Ki = 6.6 nM 8.18