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Assay Detail

CHEMBL767849

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

Binding
Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.
Tsuri T, Honma T, Hiramatsu Y, Okada T, Hashizume H, Mitsumori S, Inagaki M, Arimura A, Yasui K, Asanuma F, Kishino J, Ohtani M.
J Med Chem (1997) 40 : 3504 -3507
PubMed 9357516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.92 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116836 1 9.57
CHEMBL116837 1 9.40
CHEMBL119810 1 8.89
CHEMBL82489 1 8.07
CHEMBL119809 1 7.58
CHEMBL432935 1 7.57
CHEMBL309987 1 7.57
CHEMBL117399 1 7.50
CHEMBL119550 1 7.50
CHEMBL332635 1 7.50
CHEMBL312697 1 7.33
CHEMBL309835 1 6.89
CHEMBL325026 1 6.34
CHEMBL79360 1 6.27
CHEMBL79511 1 6.22
CHEMBL79260 1 6.14
CHEMBL82896 1 6.11
CHEMBL420398 1 5.96
CHEMBL420507 1 5.92
CHEMBL420404 1 5.89
CHEMBL419040 1 5.80
CHEMBL119397 1 5.52
CHEMBL435382 1 5.31
CHEMBL79413 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116836 IC50 = 0.27 nM 9.57
CHEMBL116837 IC50 = 0.4 nM 9.40
CHEMBL119810 IC50 = 1.3 nM 8.89
CHEMBL82489 IC50 = 8.6 nM 8.07
CHEMBL119809 IC50 = 26.0 nM 7.58
CHEMBL432935 IC50 = 27.0 nM 7.57
CHEMBL309987 IC50 = 27.0 nM 7.57
CHEMBL117399 IC50 = 32.0 nM 7.50
CHEMBL119550 IC50 = 32.0 nM 7.50
CHEMBL332635 IC50 = 32.0 nM 7.50
CHEMBL312697 IC50 = 47.0 nM 7.33
CHEMBL309835 IC50 = 130.0 nM 6.89
CHEMBL325026 IC50 = 460.0 nM 6.34
CHEMBL79360 IC50 = 540.0 nM 6.27
CHEMBL79511 IC50 = 600.0 nM 6.22
CHEMBL79260 IC50 = 720.0 nM 6.14
CHEMBL82896 IC50 = 780.0 nM 6.11
CHEMBL420398 IC50 = 1100.0 nM 5.96
CHEMBL420507 IC50 = 1200.0 nM 5.92
CHEMBL420404 IC50 = 1300.0 nM 5.89
CHEMBL419040 IC50 = 1600.0 nM 5.80
CHEMBL119397 IC50 = 3000.0 nM 5.52
CHEMBL435382 IC50 = 4900.0 nM 5.31
CHEMBL79413 IC50 = 5200.0 nM 5.28