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Assay Detail

CHEMBL695766

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Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
Meier G, Krause M, Hüls A, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem (2004) 47 : 2678 -2687
PubMed 15115409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.85 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330688 1 7.40
CHEMBL88746 1 7.01
CHEMBL88958 1 6.87
CHEMBL314526 1 6.51
CHEMBL91361 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330688 EC50 = 40.0 nM 7.40
CHEMBL88746 EC50 = 97.0 nM 7.01
CHEMBL88958 EC50 = 135.0 nM 6.87
CHEMBL314526 EC50 = 311.0 nM 6.51
CHEMBL91361 EC50 = 366.0 nM 6.44