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Assay Detail

CHEMBL5113357

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

Binding
PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type KU812 cell line
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein cereblon/Hematopoietic prostaglandin D synthase (CHEMBL4680054)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D<sub>2</sub> synthase.
Murakami Y, Osawa H, Kurohara T, Yanase Y, Ito T, Yokoo H, Shibata N, Naito M, Aritake K, Demizu Y.
RSC Med Chem (2022) 13 : 1495 -1503
PubMed 36561070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 10.52 10.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5076100 1 10.73
CHEMBL5207946 1 10.62
CHEMBL5200341 1 10.56
CHEMBL5193611 1 10.15
CHEMBL4238186 1 -
CHEMBL3650200 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5076100 EC50 = 0.0187 nM 10.73
CHEMBL5207946 EC50 = 0.0238 nM 10.62
CHEMBL5200341 EC50 = 0.0276 nM 10.56
CHEMBL5193611 EC50 = 0.0714 nM 10.15
CHEMBL4238186 EC50 - -
CHEMBL3650200 EC50 - -