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Assay Detail

CHEMBL684398

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Functional
Tested for concentration required to inhibit H1 histamine -induced guinea pig ileum contraction
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 1 — Organism
Curated By Expert

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
Carceller E, Merlos M, Giral M, Balsa D, Almansa C, Bartrolí J, García-Rafanell J, Forn J.
J Med Chem (1994) 37 : 2697 -2703
PubMed 7914928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.95 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91397 RUPATADINE 4.0 1 8.41
CHEMBL544552 1 7.43
CHEMBL90893 1 7.03
CHEMBL555304 1 6.72
CHEMBL91729 1 6.57
CHEMBL88343 1 6.55
CHEMBL92108 1 6.46
CHEMBL544551 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91397 RUPATADINE IC50 = 3.9 nM 8.41
CHEMBL544552 IC50 = 37.0 nM 7.43
CHEMBL90893 IC50 = 93.0 nM 7.03
CHEMBL555304 IC50 = 190.0 nM 6.72
CHEMBL91729 IC50 = 270.0 nM 6.57
CHEMBL88343 IC50 = 280.0 nM 6.55
CHEMBL92108 IC50 = 350.0 nM 6.46
CHEMBL544551 IC50 = 360.0 nM 6.44