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Assay Detail

CHEMBL835744

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

Functional
Inhibition of beta-arrestin translocation at human chemoattractant receptor-homologous molecule expressed on TH2 cells in BRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TH2
Confidence 9 — Direct single protein target
Curated By Expert

Target

Prostaglandin D2 receptor 2 (CHEMBL5071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Ulven T, Kostenis E.
J Med Chem (2005) 48 : 897 -900
PubMed 15715457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.08 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179036 1 8.52
CHEMBL194085 1 8.42
CHEMBL373118 1 7.82
CHEMBL361812 RAMATROBAN 4.0 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179036 IC50 = 3.0 nM 8.52
CHEMBL194085 IC50 = 3.8 nM 8.42
CHEMBL373118 IC50 = 15.0 nM 7.82
CHEMBL361812 RAMATROBAN IC50 = 28.0 nM 7.55