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Assay Detail

CHEMBL4005281

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

Binding
Displacement of [3H]-PGD2 from recombinant human DP1 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor (CHEMBL4427)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Tran TA, Kramer B, Shin YJ, Vallar P, Boatman PD, Zou N, Sage CR, Gharbaoui T, Krishnan A, Pal B, Shakya SR, Garrido Montalban A, Adams JW, Ramirez J, Behan DP, Shifrina A, Blackburn A, Leakakos T, Shi Y, Morgan M, Sadeque A, Chen W, Unett DJ, Gaidarov I, Chen X, Chang S, Shu HH, Tung SF, Semple G.
J Med Chem (2017) 60 : 913 -927
PubMed 28072531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.66 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3933704 1 5.73
CHEMBL3301604 RALINEPAG 3.0 1 5.58
CHEMBL494 ILOPROST 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3933704 Ki = 1850.0 nM 5.73
CHEMBL3301604 RALINEPAG Ki = 2600.0 nM 5.58
CHEMBL494 ILOPROST Ki - -