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Assay Detail

CHEMBL5133047

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

Functional
Antagonist activity against human CysLT1 expressed in CHO cells assessed as inhibition of LTD4 induced cytosolic Calcium ion mobilization measured after 75 mins by Fluo4 dye based fluorimetric microplate reader assay relative to control
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cysteinyl leukotriene receptor 1 (CHEMBL1798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.
Fiorillo B, Sepe V, Conflitti P, Roselli R, Biagioli M, Marchianò S, De Luca P, Baronissi G, Rapacciuolo P, Cassiano C, Catalanotti B, Zampella A, Limongelli V, Fiorucci S.
J Med Chem (2021) 64 : 16512 -16529
PubMed 34767347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.55 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8747 REV-5901 1 5.96
CHEMBL5174405 1 5.92
CHEMBL5181326 1 5.68
CHEMBL5169385 1 5.55
CHEMBL5173307 1 5.41
CHEMBL5189181 1 5.29
CHEMBL5192002 1 5.02
CHEMBL5205902 1 -
CHEMBL5202995 1 -
CHEMBL5193617 1 -
CHEMBL5185938 1 -
CHEMBL5177797 1 -
CHEMBL5189686 1 -
CHEMBL18775 1 -
CHEMBL5173976 1 -
CHEMBL5172427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8747 REV-5901 IC50 = 1100.0 nM 5.96
CHEMBL5174405 IC50 = 1200.0 nM 5.92
CHEMBL5181326 IC50 = 2100.0 nM 5.68
CHEMBL5169385 IC50 = 2800.0 nM 5.55
CHEMBL5173307 IC50 = 3900.0 nM 5.41
CHEMBL5189181 IC50 = 5110.0 nM 5.29
CHEMBL5192002 IC50 = 9630.0 nM 5.02
CHEMBL5205902 IC50 - -
CHEMBL5202995 IC50 - -
CHEMBL5193617 IC50 - -
CHEMBL5185938 IC50 - -
CHEMBL5177797 IC50 - -
CHEMBL5189686 IC50 - -
CHEMBL18775 IC50 - -
CHEMBL5173976 IC50 - -
CHEMBL5172427 IC50 - -