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Assay Detail

CHEMBL768433

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

Binding
Prostaglandin I2 receptor binding by displacement of [3H]iloprost from human platelets
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostacyclin receptor (CHEMBL1995)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular design of novel PGI2 agonists without PG skeleton. I
Hamanaka N, Takahashi K, Nagao Y, Torisu K, Tokumoto H, Kondo K
Bioorg Med Chem Lett (1995) 5 : 1065 -1070
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.62 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494 ILOPROST 4.0 1 7.57
CHEMBL10470 1 6.22
CHEMBL10742 1 6.19
CHEMBL10442 1 5.52
CHEMBL10856 1 5.51
CHEMBL10261 1 5.41
CHEMBL10564 1 5.31
CHEMBL275493 1 5.28
CHEMBL10740 1 5.11
CHEMBL10439 1 5.02
CHEMBL10404 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494 ILOPROST IC50 = 27.0 nM 7.57
CHEMBL10470 IC50 = 600.0 nM 6.22
CHEMBL10742 IC50 = 650.0 nM 6.19
CHEMBL10442 IC50 = 3000.0 nM 5.52
CHEMBL10856 IC50 = 3100.0 nM 5.51
CHEMBL10261 IC50 = 3900.0 nM 5.41
CHEMBL10564 IC50 = 4900.0 nM 5.31
CHEMBL275493 IC50 = 5300.0 nM 5.28
CHEMBL10740 IC50 = 7800.0 nM 5.11
CHEMBL10439 IC50 = 9600.0 nM 5.02
CHEMBL10404 IC50 = 23000.0 nM 4.64