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Assay Detail

CHEMBL928087

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

Binding
Inhibition of glutathione-S-transferase activity of prostaglandin D2 synthase
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel prostaglandin D synthase inhibitors generated by fragment-based drug design.
Hohwy M, Spadola L, Lundquist B, Hawtin P, Dahmén J, Groth-Clausen I, Nilsson E, Persdotter S, von Wachenfeldt K, Folmer RH, Edman K.
J Med Chem (2008) 51 : 2178 -2186
PubMed 18341273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.37 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261777 1 7.68
CHEMBL258506 1 7.12
CHEMBL258467 1 6.86
CHEMBL265720 1 6.04
CHEMBL264951 1 6.00
CHEMBL442461 1 5.82
CHEMBL261693 1 5.42
CHEMBL127757 1 5.42
CHEMBL415324 TRANILAST 3.0 1 4.94
CHEMBL260489 1 4.91
CHEMBL261678 1 4.76
CHEMBL408265 1 4.58
CHEMBL405844 1 4.48
CHEMBL260289 1 4.46
CHEMBL260488 1 4.35
CHEMBL406105 1 3.05
CHEMBL264950 1 -
CHEMBL263379 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261777 IC50 = 21.0 nM 7.68
CHEMBL258506 IC50 = 75.0 nM 7.12
CHEMBL258467 IC50 = 138.0 nM 6.86
CHEMBL265720 IC50 = 920.0 nM 6.04
CHEMBL264951 IC50 = 994.0 nM 6.00
CHEMBL442461 IC50 = 1500.0 nM 5.82
CHEMBL261693 IC50 = 3800.0 nM 5.42
CHEMBL127757 IC50 = 3800.0 nM 5.42
CHEMBL415324 TRANILAST IC50 = 11600.0 nM 4.94
CHEMBL260489 IC50 = 12400.0 nM 4.91
CHEMBL261678 IC50 = 17400.0 nM 4.76
CHEMBL408265 IC50 = 26400.0 nM 4.58
CHEMBL405844 IC50 = 33000.0 nM 4.48
CHEMBL260289 IC50 = 34700.0 nM 4.46
CHEMBL260488 IC50 = 45000.0 nM 4.35
CHEMBL406105 IC50 = 890000.0 nM 3.05
CHEMBL264950 IC50 - -
CHEMBL263379 IC50 - -