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Assay Detail

CHEMBL1815366

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

Functional
Antagonist activity at mouse DP receptor expressed in CHO cells assessed as inhibition of PGD2-induced cAMP accumulation after 10 mins by enzyme immunoassay in the presence of 0.1% BSA
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 selective indole-based prostaglandin D₂ receptor antagonist.
Iwahashi M, Shimabukuro A, Onoda T, Matsunaga Y, Okada Y, Matsumoto R, Nambu F, Nakai H, Toda M.
Bioorg Med Chem (2011) 19 : 4574 -4588
PubMed 21737285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.30 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1813277 1 9.15
CHEMBL1813120 1 8.96
CHEMBL1813276 1 8.80
CHEMBL1813289 1 8.74
CHEMBL1813118 1 8.74
CHEMBL1813287 1 8.66
CHEMBL1813121 1 8.66
CHEMBL364841 1 8.62
CHEMBL1813122 1 8.60
CHEMBL1813281 1 8.55
CHEMBL1813288 1 8.51
CHEMBL1813117 1 8.51
CHEMBL1813275 1 8.49
CHEMBL1813282 1 8.42
CHEMBL1813116 1 8.37
CHEMBL1813286 1 8.21
CHEMBL1813284 1 8.15
CHEMBL1813280 1 7.50
CHEMBL1813278 1 7.38
CHEMBL1813285 1 7.37
CHEMBL1813279 1 7.17
CHEMBL1813283 1 7.14
CHEMBL1813119 1 -
CHEMBL1813274 1 -
CHEMBL1813273 1 -
CHEMBL1813272 1 -
CHEMBL1813115 1 -
CHEMBL1813125 1 -
CHEMBL1813124 1 -
CHEMBL1813123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1813277 IC50 = 0.7 nM 9.15
CHEMBL1813120 IC50 = 1.1 nM 8.96
CHEMBL1813276 IC50 = 1.6 nM 8.80
CHEMBL1813289 IC50 = 1.8 nM 8.74
CHEMBL1813118 IC50 = 1.8 nM 8.74
CHEMBL1813287 IC50 = 2.2 nM 8.66
CHEMBL1813121 IC50 = 2.2 nM 8.66
CHEMBL364841 IC50 = 2.4 nM 8.62
CHEMBL1813122 IC50 = 2.5 nM 8.60
CHEMBL1813281 IC50 = 2.8 nM 8.55
CHEMBL1813288 IC50 = 3.1 nM 8.51
CHEMBL1813117 IC50 = 3.1 nM 8.51
CHEMBL1813275 IC50 = 3.2 nM 8.49
CHEMBL1813282 IC50 = 3.8 nM 8.42
CHEMBL1813116 IC50 = 4.3 nM 8.37
CHEMBL1813286 IC50 = 6.2 nM 8.21
CHEMBL1813284 IC50 = 7.0 nM 8.15
CHEMBL1813280 IC50 = 32.0 nM 7.50
CHEMBL1813278 IC50 = 42.0 nM 7.38
CHEMBL1813285 IC50 = 43.0 nM 7.37
CHEMBL1813279 IC50 = 68.0 nM 7.17
CHEMBL1813283 IC50 = 72.0 nM 7.14
CHEMBL1813119 IC50 - -
CHEMBL1813274 IC50 - -
CHEMBL1813273 IC50 - -
CHEMBL1813272 IC50 - -
CHEMBL1813115 IC50 - -
CHEMBL1813125 IC50 - -
CHEMBL1813124 IC50 - -
CHEMBL1813123 IC50 - -
CHEMBL6 INDOMETHACIN IC50 - -