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Assay Detail

CHEMBL5265294

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

Binding
Binding affinity to human H-PGDS expressed in Escherichia coli BL21 DE3 cells assessed as equilibrium dissociation constant by measuring changes in intrinsic tryptophan fluorescence in presence of glutathione by fluorescence based analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hematopoietic prostaglandin D synthase (CHEMBL5879)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA.
Bioorg Med Chem (2020) 28 : 115791 -115791
PubMed 33059303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.62 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5285108 1 9.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5285108 Kd = 0.24 nM 9.62