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Assay Detail

CHEMBL3241469

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

Binding
Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.
Savall BM, Chavez F, Tays K, Dunford PJ, Cowden JM, Hack MD, Wolin RL, Thurmond RL, Edwards JP.
J Med Chem (2014) 57 : 2429 -2439
PubMed 24495018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.59 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236553 1 7.62
CHEMBL3236568 1 6.17
CHEMBL3236549 JNJ-39758979 2.0 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236553 Ki = 24.0 nM 7.62
CHEMBL3236568 Ki = 670.0 nM 6.17
CHEMBL3236549 JNJ-39758979 Ki = 1043.0 nM 5.98