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Assay Detail

CHEMBL1918136

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

Functional
Antagonist activity at mouse prostanoid DP receptor expressed in CHO cells assessed as inhibition of PGD2-induced intracellular cAMP production after 10 mins by enzyme immunoassay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor (CHEMBL3933)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of new orally active prostaglandin D2 receptor antagonists.
Iwahashi M, Naganawa A, Kinoshita A, Shimabukuro A, Nishiyama T, Ogawa S, Matsunaga Y, Tsukamoto K, Okada Y, Matsumoto R, Nambu F, Oumi R, Odagaki Y, Katagi J, Yano K, Tani K, Nakai H, Toda M.
Bioorg Med Chem (2011) 19 : 6935 -6948
PubMed 21982795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.12 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915863 1 9.15
CHEMBL1915865 1 9.00
CHEMBL1915866 1 8.85
CHEMBL1915858 1 8.82
CHEMBL1819615 1 8.74
CHEMBL364841 1 8.62
CHEMBL1819608 1 8.48
CHEMBL1915672 1 8.46
CHEMBL1819622 1 8.37
CHEMBL1915857 1 8.37
CHEMBL1819611 1 8.34
CHEMBL1915675 1 8.32
CHEMBL1915677 1 8.29
CHEMBL1915674 1 8.24
CHEMBL1819619 1 8.22
CHEMBL1915861 1 8.15
CHEMBL1819623 1 8.13
CHEMBL1915856 1 8.12
CHEMBL1915673 1 7.92
CHEMBL1915859 1 7.85
CHEMBL1819609 1 7.70
CHEMBL1915670 1 7.66
CHEMBL1915867 1 7.62
CHEMBL1915864 1 7.58
CHEMBL1915860 1 7.57
CHEMBL1915671 1 7.55
CHEMBL1915862 1 7.37
CHEMBL1915676 1 7.27
CHEMBL1819603 1 6.66
CHEMBL1915669 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915863 IC50 = 0.7 nM 9.15
CHEMBL1915865 IC50 = 1.0 nM 9.00
CHEMBL1915866 IC50 = 1.4 nM 8.85
CHEMBL1915858 IC50 = 1.5 nM 8.82
CHEMBL1819615 IC50 = 1.8 nM 8.74
CHEMBL364841 IC50 = 2.4 nM 8.62
CHEMBL1819608 IC50 = 3.3 nM 8.48
CHEMBL1915672 IC50 = 3.5 nM 8.46
CHEMBL1819622 IC50 = 4.3 nM 8.37
CHEMBL1915857 IC50 = 4.3 nM 8.37
CHEMBL1819611 IC50 = 4.6 nM 8.34
CHEMBL1915675 IC50 = 4.8 nM 8.32
CHEMBL1915677 IC50 = 5.1 nM 8.29
CHEMBL1915674 IC50 = 5.7 nM 8.24
CHEMBL1819619 IC50 = 6.0 nM 8.22
CHEMBL1915861 IC50 = 7.0 nM 8.15
CHEMBL1819623 IC50 = 7.4 nM 8.13
CHEMBL1915856 IC50 = 7.6 nM 8.12
CHEMBL1915673 IC50 = 12.0 nM 7.92
CHEMBL1915859 IC50 = 14.0 nM 7.85
CHEMBL1819609 IC50 = 20.0 nM 7.70
CHEMBL1915670 IC50 = 22.0 nM 7.66
CHEMBL1915867 IC50 = 24.0 nM 7.62
CHEMBL1915864 IC50 = 26.0 nM 7.58
CHEMBL1915860 IC50 = 27.0 nM 7.57
CHEMBL1915671 IC50 = 28.0 nM 7.55
CHEMBL1915862 IC50 = 43.0 nM 7.37
CHEMBL1915676 IC50 = 54.0 nM 7.27
CHEMBL1819603 IC50 = 220.0 nM 6.66
CHEMBL1915669 IC50 - -
CHEMBL1819614 IC50 - -