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Assay Detail

CHEMBL3428604

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

Binding
Inhibition human HPGDS expressed in Escherichia coli assessed as reduction in GST enzymatic activity using MCBL and glutathione incubated for 30 mins by fluorescence based assay
20
Total Activities
20
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

Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS).
Edfeldt F, Evenäs J, Lepistö M, Ward A, Petersen J, Wissler L, Rohman M, Sivars U, Svensson K, Perry M, Feierberg I, Zhou XH, Hansson T, Narjes F.
Bioorg Med Chem Lett (2015) 25 : 2496 -2500
PubMed 25978964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.00 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261777 1 7.64
CHEMBL3425953 1 7.58
CHEMBL3425959 1 7.51
CHEMBL3425954 1 7.50
CHEMBL3425955 1 7.46
CHEMBL3425956 1 7.37
CHEMBL3425960 1 7.32
CHEMBL3425948 1 7.22
CHEMBL3425966 1 7.16
CHEMBL3425949 1 7.16
CHEMBL3425968 1 7.15
CHEMBL3425957 1 6.89
CHEMBL3425952 1 6.77
CHEMBL3425950 1 6.75
CHEMBL1233897 1 6.70
CHEMBL3425961 1 6.64
CHEMBL3425951 1 6.52
CHEMBL3425963 1 6.50
CHEMBL3425965 1 6.23
CHEMBL3425958 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261777 IC50 = 23.0 nM 7.64
CHEMBL3425953 IC50 = 26.0 nM 7.58
CHEMBL3425959 IC50 = 31.0 nM 7.51
CHEMBL3425954 IC50 = 32.0 nM 7.50
CHEMBL3425955 IC50 = 35.0 nM 7.46
CHEMBL3425956 IC50 = 43.0 nM 7.37
CHEMBL3425960 IC50 = 48.0 nM 7.32
CHEMBL3425948 IC50 = 60.0 nM 7.22
CHEMBL3425966 IC50 = 70.0 nM 7.16
CHEMBL3425949 IC50 = 70.0 nM 7.16
CHEMBL3425968 IC50 = 71.0 nM 7.15
CHEMBL3425957 IC50 = 130.0 nM 6.89
CHEMBL3425952 IC50 = 170.0 nM 6.77
CHEMBL3425950 IC50 = 180.0 nM 6.75
CHEMBL1233897 IC50 = 200.0 nM 6.70
CHEMBL3425961 IC50 = 230.0 nM 6.64
CHEMBL3425951 IC50 = 300.0 nM 6.52
CHEMBL3425963 IC50 = 320.0 nM 6.50
CHEMBL3425965 IC50 = 590.0 nM 6.23
CHEMBL3425958 IC50 = 1200.0 nM 5.92