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Assay Detail

CHEMBL912671

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Functional
Agonist activity at human PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostacyclin receptor (CHEMBL1995)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
Tanaka A, Hattori K, Taniguchi K, Okitsu O, Tabuchi S, Nishio M, Nagakura Y, Maeda N, Murai H, Seki J.
Bioorg Med Chem Lett (2006) 16 : 4861 -4864
PubMed 16837197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.96 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215442 1 7.41
CHEMBL439357 1 7.32
CHEMBL379203 1 7.28
CHEMBL438092 1 7.24
CHEMBL132589 1 7.22
CHEMBL212943 1 6.94
CHEMBL405770 1 6.94
CHEMBL132649 1 6.27
CHEMBL386580 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215442 IC50 = 39.0 nM 7.41
CHEMBL439357 IC50 = 48.0 nM 7.32
CHEMBL379203 IC50 = 53.0 nM 7.28
CHEMBL438092 IC50 = 58.0 nM 7.24
CHEMBL132589 IC50 = 60.0 nM 7.22
CHEMBL212943 IC50 = 114.0 nM 6.94
CHEMBL405770 IC50 = 115.0 nM 6.94
CHEMBL132649 IC50 = 533.0 nM 6.27
CHEMBL386580 IC50 = 930.0 nM 6.03