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Assay Detail

CHEMBL768446

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

Binding
In vitro inhibition of Prostaglandin I2 synthase from human blood platelet microsomes
41
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostacyclin synthase (CHEMBL4428)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids.
Faull AW, Brewster AG, Brown GR, Smithers MJ, Jackson R.
J Med Chem (1995) 38 : 686 -694
PubMed 7861416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 4.93 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159876 1 5.70
CHEMBL163278 1 5.70
CHEMBL350510 1 5.70
CHEMBL355596 1 5.60
CHEMBL161608 1 5.52
CHEMBL159859 3 5.47
CHEMBL162406 1 5.40
CHEMBL161357 1 5.40
CHEMBL159778 1 5.30
CHEMBL159851 1 5.16
CHEMBL161911 1 5.16
CHEMBL159737 1 5.10
CHEMBL422719 1 5.05
CHEMBL159243 1 5.05
CHEMBL445644 2 4.92
CHEMBL346590 1 4.89
CHEMBL159571 1 4.89
CHEMBL159268 1 4.85
CHEMBL423248 1 4.64
CHEMBL350595 1 4.60
CHEMBL352668 2 4.55
CHEMBL161304 1 4.50
CHEMBL161063 1 4.43
CHEMBL435049 1 4.40
CHEMBL162032 1 4.29
CHEMBL158687 1 4.22
CHEMBL159344 1 4.14
CHEMBL159196 1 4.12
CHEMBL353356 1 -
CHEMBL161104 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL163278 IC50 = 2000.0 nM 5.70
CHEMBL350510 IC50 = 2000.0 nM 5.70
CHEMBL159876 IC50 = 2000.0 nM 5.70
CHEMBL355596 IC50 = 2500.0 nM 5.60
CHEMBL161608 IC50 = 3000.0 nM 5.52
CHEMBL159859 IC50 = 3400.0 nM 5.47
CHEMBL162406 IC50 = 4000.0 nM 5.40
CHEMBL161357 IC50 = 4000.0 nM 5.40
CHEMBL159859 IC50 = 4000.0 nM 5.40
CHEMBL159778 IC50 = 5000.0 nM 5.30
CHEMBL159851 IC50 = 7000.0 nM 5.16
CHEMBL161911 IC50 = 7000.0 nM 5.16
CHEMBL159737 IC50 = 8000.0 nM 5.10
CHEMBL422719 IC50 = 9000.0 nM 5.05
CHEMBL159243 IC50 = 9000.0 nM 5.05
CHEMBL445644 IC50 = 12000.0 nM 4.92
CHEMBL159571 IC50 = 13000.0 nM 4.89
CHEMBL346590 IC50 = 13000.0 nM 4.89
CHEMBL159268 IC50 = 14000.0 nM 4.85
CHEMBL423248 IC50 = 23000.0 nM 4.64
CHEMBL350595 IC50 = 25000.0 nM 4.60
CHEMBL352668 IC50 = 28000.0 nM 4.55
CHEMBL161304 IC50 = 32000.0 nM 4.50
CHEMBL352668 IC50 = 33000.0 nM 4.48
CHEMBL161063 IC50 = 37000.0 nM 4.43
CHEMBL435049 IC50 = 40000.0 nM 4.40
CHEMBL445644 IC50 = 47000.0 nM 4.33
CHEMBL162032 IC50 = 51000.0 nM 4.29
CHEMBL158687 IC50 = 60000.0 nM 4.22
CHEMBL159344 IC50 = 73000.0 nM 4.14
CHEMBL159196 IC50 = 75000.0 nM 4.12
CHEMBL159699 IC50 > 100000.0 nM -
CHEMBL159859 IC50 < 1000.0 nM -
CHEMBL348968 IC50 > 100000.0 nM -
CHEMBL350816 IC50 > 100000.0 nM -
CHEMBL26820 (E)-ISBOGREL IC50 > 100000.0 nM -
CHEMBL352196 IC50 > 100000.0 nM -
CHEMBL161518 IC50 < 1000.0 nM -
CHEMBL353356 IC50 < 1000.0 nM -
CHEMBL161104 IC50 > 100000.0 nM -
CHEMBL352075 IC50 > 100000.0 nM -