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Assay Detail

CHEMBL693827

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Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Conformationally-restricted ligands for the histamine H1 receptor.
Upton C, Osborne RH, Jaffar M.
Bioorg Med Chem Lett (2000) 10 : 1277 -1279
PubMed 10866399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.37 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280432 1 7.97
CHEMBL23897 1 7.77
CHEMBL283169 1 7.64
CHEMBL23638 1 7.58
CHEMBL22215 1 7.55
CHEMBL511 PYRILAMINE 4.0 1 7.47
CHEMBL278398 PHENINDAMINE 2.0 1 7.44
CHEMBL279297 1 7.28
CHEMBL281638 1 6.66
CHEMBL279454 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280432 IC50 = 10.8 nM 7.97
CHEMBL23897 IC50 = 17.0 nM 7.77
CHEMBL283169 IC50 = 23.0 nM 7.64
CHEMBL23638 IC50 = 26.0 nM 7.58
CHEMBL22215 IC50 = 28.0 nM 7.55
CHEMBL511 PYRILAMINE IC50 = 34.0 nM 7.47
CHEMBL278398 PHENINDAMINE IC50 = 36.0 nM 7.44
CHEMBL279297 IC50 = 53.0 nM 7.28
CHEMBL281638 IC50 = 220.0 nM 6.66
CHEMBL279454 IC50 = 470.0 nM 6.33