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Assay Detail

CHEMBL4236045

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

Binding
Inhibition of HPGDS (unknown origin)
7
Total Activities
7
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

Amelioration of mechanism-based inactivation of CYP3A4 by a H-PGDS inhibitor.
Vaz RJ, Li Y, Munson M, Elliot M, Thurairatnam S.
Bioorg Med Chem Lett (2018) 28 : 3046 -3049
PubMed 30115511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.09 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4247050 1 8.52
CHEMBL4241885 1 8.22
CHEMBL3181890 1 8.15
CHEMBL4250602 1 8.10
CHEMBL4242281 1 8.02
CHEMBL4239352 1 8.00
CHEMBL4244590 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4247050 IC50 = 3.0 nM 8.52
CHEMBL4241885 IC50 = 6.0 nM 8.22
CHEMBL3181890 IC50 = 7.0 nM 8.15
CHEMBL4250602 IC50 = 8.0 nM 8.10
CHEMBL4242281 IC50 = 9.5 nM 8.02
CHEMBL4239352 IC50 = 10.0 nM 8.00
CHEMBL4244590 IC50 = 23.0 nM 7.64