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Assay Detail

CHEMBL693458

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Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.
Sasse A, Stark H, Reidemeister S, Hüls A, Elz S, Ligneau X, Ganellin CR, Schwartz JC, Schunack W.
J Med Chem (1999) 42 : 4269 -4274
PubMed 10514298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.60 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19439 IMETIT 1 8.55
CHEMBL2145443 1 7.35
CHEMBL2145444 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19439 IMETIT EC50 = 2.8 nM 8.55
CHEMBL2145443 EC50 = 45.0 nM 7.35
CHEMBL2145444 EC50 = 128.0 nM 6.89