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Assay Detail

CHEMBL768434

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

Binding
Displacement of [3H]iloprost from Prostaglandin I2 receptor of 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. II
Hamanaka N, Takahashi K, Nagao Y, Torisu K, Takada H, Tokumoto H, Kondo K
Bioorg Med Chem Lett (1995) 5 : 1071 -1076
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.29 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494 ILOPROST 4.0 1 7.57
CHEMBL268477 AP-227 1 6.82
CHEMBL416334 1 6.82
CHEMBL268051 1 6.66
CHEMBL11088 1 6.42
CHEMBL10470 1 6.22
CHEMBL10742 1 6.19
CHEMBL495 ALPROSTADIL 4.0 1 5.85
CHEMBL10829 1 5.68
CHEMBL418338 1 5.66
CHEMBL10853 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494 ILOPROST IC50 = 27.0 nM 7.57
CHEMBL268477 AP-227 IC50 = 150.0 nM 6.82
CHEMBL416334 IC50 = 150.0 nM 6.82
CHEMBL268051 IC50 = 220.0 nM 6.66
CHEMBL11088 IC50 = 380.0 nM 6.42
CHEMBL10470 IC50 = 600.0 nM 6.22
CHEMBL10742 IC50 = 650.0 nM 6.19
CHEMBL495 ALPROSTADIL IC50 = 1400.0 nM 5.85
CHEMBL10829 IC50 = 2100.0 nM 5.68
CHEMBL418338 IC50 = 2200.0 nM 5.66
CHEMBL10853 IC50 = 5300.0 nM 5.28