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Assay Detail

CHEMBL687399

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

Functional
Ex vivo inhibition of LTD4 induced contraction of guinea pig ileum.
5
Total Activities
5
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

Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.
Zwaagstra ME, Timmerman H, van de Stolpe AC, de Kanter FJ, Tamura M, Wada Y, Zhang MQ.
J Med Chem (1998) 41 : 1428 -1438
PubMed 9554876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.39 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416769 1 7.82
CHEMBL34835 1 7.55
CHEMBL284624 1 7.38
CHEMBL32138 1 7.21
CHEMBL32136 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416769 IC50 = 15.0 nM 7.82
CHEMBL34835 IC50 = 28.0 nM 7.55
CHEMBL284624 IC50 = 42.0 nM 7.38
CHEMBL32138 IC50 = 61.0 nM 7.21
CHEMBL32136 IC50 = 100.0 nM 7.00