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Assay Detail

CHEMBL767848

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

Binding
In vitro inhibition of [3H]- PGD-2 radioligand binding to prostaglandin D2 receptor on human platelet membrane
ChEMBL ↗
47
Total Activities
47
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

Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.
Mitsumori S, Tsuri T, Honma T, Hiramatsu Y, Okada T, Hashizume H, Inagaki M, Arimura A, Yasui K, Asanuma F, Kishino J, Ohtani M.
J Med Chem (2003) 46 : 2436 -2445
PubMed 12773047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.63 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82489 — — 1 8.07
CHEMBL311199 — — 1 7.82
CHEMBL78904 — — 1 7.75
CHEMBL312715 — — 1 7.66
CHEMBL79669 — — 1 7.66
CHEMBL309987 — — 1 7.62
CHEMBL432935 — — 1 7.60
CHEMBL81185 — — 1 7.50
CHEMBL430627 — — 1 7.47
CHEMBL82426 — — 1 7.44
CHEMBL309443 — — 1 7.38
CHEMBL312697 — — 1 7.33
CHEMBL309999 — — 1 7.24
CHEMBL413523 — — 1 7.21
CHEMBL312983 — — 1 7.19
CHEMBL81600 — — 1 7.05
CHEMBL82537 — — 1 7.00
CHEMBL78939 — — 1 6.92
CHEMBL309835 — — 1 6.89
CHEMBL311105 — — 1 6.75
CHEMBL310301 — — 1 6.72
CHEMBL79095 — — 1 6.72
CHEMBL310505 — — 1 6.70
CHEMBL2114171 — — 1 6.70
CHEMBL83269 — — 1 6.48
CHEMBL79320 — — 1 6.42
CHEMBL311038 — — 1 6.39
CHEMBL420777 — — 1 6.35
CHEMBL310643 — — 1 6.26
CHEMBL420398 — — 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82489 — IC50 = 8.5 nM 8.07
CHEMBL311199 — IC50 = 15.0 nM 7.82
CHEMBL78904 — IC50 = 18.0 nM 7.75
CHEMBL312715 — IC50 = 22.0 nM 7.66
CHEMBL79669 — IC50 = 22.0 nM 7.66
CHEMBL309987 — IC50 = 24.0 nM 7.62
CHEMBL432935 — IC50 = 25.0 nM 7.60
CHEMBL81185 — IC50 = 32.0 nM 7.50
CHEMBL430627 — IC50 = 34.0 nM 7.47
CHEMBL82426 — IC50 = 36.0 nM 7.44
CHEMBL309443 — IC50 = 42.0 nM 7.38
CHEMBL312697 — IC50 = 47.0 nM 7.33
CHEMBL309999 — IC50 = 57.0 nM 7.24
CHEMBL413523 — IC50 = 62.0 nM 7.21
CHEMBL312983 — IC50 = 64.0 nM 7.19
CHEMBL81600 — IC50 = 90.0 nM 7.05
CHEMBL82537 — IC50 = 100.0 nM 7.00
CHEMBL78939 — IC50 = 120.0 nM 6.92
CHEMBL309835 — IC50 = 130.0 nM 6.89
CHEMBL311105 — IC50 = 180.0 nM 6.75
CHEMBL310301 — IC50 = 190.0 nM 6.72
CHEMBL79095 — IC50 = 190.0 nM 6.72
CHEMBL2114171 — IC50 = 200.0 nM 6.70
CHEMBL310505 — IC50 = 200.0 nM 6.70
CHEMBL83269 — IC50 = 330.0 nM 6.48
CHEMBL79320 — IC50 = 380.0 nM 6.42
CHEMBL311038 — IC50 = 410.0 nM 6.39
CHEMBL420777 — IC50 = 450.0 nM 6.35
CHEMBL310643 — IC50 = 550.0 nM 6.26
CHEMBL420398 — IC50 = 550.0 nM 6.26
CHEMBL310454 — IC50 = 580.0 nM 6.24
CHEMBL79511 — IC50 = 600.0 nM 6.22
CHEMBL311769 — IC50 = 660.0 nM 6.18
CHEMBL83893 — IC50 = 670.0 nM 6.17
CHEMBL79260 — IC50 = 680.0 nM 6.17
CHEMBL312182 — IC50 = 680.0 nM 6.17
CHEMBL312707 — IC50 = 960.0 nM 6.02
CHEMBL309752 — IC50 = 1100.0 nM 5.96
CHEMBL312834 — IC50 = 5200.0 nM 5.28
CHEMBL81050 — IC50 = 5300.0 nM 5.28
CHEMBL81804 — IC50 = 5400.0 nM 5.27
CHEMBL81751 — IC50 = 5400.0 nM 5.27
CHEMBL81768 — IC50 = 6000.0 nM 5.22
CHEMBL81757 — IC50 = 8600.0 nM 5.07
CHEMBL83485 — IC50 = 8600.0 nM 5.07
CHEMBL79522 — IC50 > 10000.0 nM -
CHEMBL309847 — IC50 > 10000.0 nM -