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Assay Detail

CHEMBL768775

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

Binding
Prostaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranes
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.
Mitsumori S, Tsuri T, Honma T, Hiramatsu Y, Okada T, Hashizume H, Kida S, Inagaki M, Arimura A, Yasui K, Asanuma F, Kishino J, Ohtani M.
J Med Chem (2003) 46 : 2446 -2455
PubMed 12773048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.38 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL79943 — — 1 9.38
CHEMBL311790 — — 1 8.72
CHEMBL84452 — — 1 8.66
CHEMBL81231 — — 1 7.89
CHEMBL81785 — — 1 7.72
CHEMBL84413 — — 1 7.58
CHEMBL79700 — — 1 7.50
CHEMBL420956 — — 1 7.38
CHEMBL446628 — — 1 7.33
CHEMBL83788 — — 1 6.82
CHEMBL311977 — — 1 6.75
CHEMBL81538 — — 1 6.48
CHEMBL310830 — — 1 6.38
CHEMBL79612 — — 1 6.28
CHEMBL315977 — — 1 6.28
CHEMBL79360 — — 1 6.27
CHEMBL82468 — — 1 6.25
CHEMBL312092 — — 1 6.23
CHEMBL79998 — — 1 6.16
CHEMBL82896 — — 1 6.11
CHEMBL420588 — — 1 5.92
CHEMBL312441 — — 1 5.89
CHEMBL312476 — — 1 5.89
CHEMBL420404 — — 1 5.89
CHEMBL79972 — — 1 5.80
CHEMBL79941 — — 1 5.68
CHEMBL420953 — — 1 5.48
CHEMBL311999 — — 1 5.47
CHEMBL79424 — — 1 5.44
CHEMBL310304 — — 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL79943 — IC50 = 0.42 nM 9.38
CHEMBL311790 — IC50 = 1.9 nM 8.72
CHEMBL84452 — IC50 = 2.2 nM 8.66
CHEMBL81231 — IC50 = 13.0 nM 7.89
CHEMBL81785 — IC50 = 19.0 nM 7.72
CHEMBL84413 — IC50 = 26.0 nM 7.58
CHEMBL79700 — IC50 = 32.0 nM 7.50
CHEMBL420956 — IC50 = 42.0 nM 7.38
CHEMBL446628 — IC50 = 47.0 nM 7.33
CHEMBL83788 — IC50 = 150.0 nM 6.82
CHEMBL311977 — IC50 = 180.0 nM 6.75
CHEMBL81538 — IC50 = 330.0 nM 6.48
CHEMBL310830 — IC50 = 420.0 nM 6.38
CHEMBL79612 — IC50 = 520.0 nM 6.28
CHEMBL315977 — IC50 = 520.0 nM 6.28
CHEMBL79360 — IC50 = 540.0 nM 6.27
CHEMBL82468 — IC50 = 560.0 nM 6.25
CHEMBL312092 — IC50 = 590.0 nM 6.23
CHEMBL79998 — IC50 = 690.0 nM 6.16
CHEMBL82896 — IC50 = 780.0 nM 6.11
CHEMBL420588 — IC50 = 1200.0 nM 5.92
CHEMBL312441 — IC50 = 1300.0 nM 5.89
CHEMBL420404 — IC50 = 1300.0 nM 5.89
CHEMBL312476 — IC50 = 1300.0 nM 5.89
CHEMBL79972 — IC50 = 1600.0 nM 5.80
CHEMBL79941 — IC50 = 2100.0 nM 5.68
CHEMBL420953 — IC50 = 3300.0 nM 5.48
CHEMBL311999 — IC50 = 3400.0 nM 5.47
CHEMBL79424 — IC50 = 3600.0 nM 5.44
CHEMBL310304 — IC50 = 3900.0 nM 5.41
CHEMBL81654 — IC50 = 4400.0 nM 5.36
CHEMBL80002 — IC50 = 4500.0 nM 5.35
CHEMBL81004 — IC50 = 4600.0 nM 5.34
CHEMBL79370 — IC50 = 5100.0 nM 5.29
CHEMBL79413 — IC50 = 5200.0 nM 5.28
CHEMBL81338 — IC50 = 6000.0 nM 5.22
CHEMBL312216 — IC50 = 7500.0 nM 5.12
CHEMBL81746 — IC50 > 10000.0 nM -
CHEMBL81339 — IC50 > 10000.0 nM -
CHEMBL83776 — IC50 > 10000.0 nM -
CHEMBL79773 — IC50 > 10000.0 nM -
CHEMBL79843 — IC50 > 10000.0 nM -
CHEMBL310218 — IC50 > 10000.0 nM -