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Assay Detail

CHEMBL4427800

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

Binding
Inhibition of CENP-E in human HeLa cells assessed as HH3 phosphorylated levels after 24 hrs by FACS analysis
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Centromere-associated protein E (CHEMBL5870)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of fused bicyclic inhibitors targeting the L5 loop site of centromere-associated protein E.
Hirayama T, Okaniwa M, Banno H, Kakei H, Ohashi A, Ohori M, Nambu T, Iwai K, Kawamoto T, Yokota A, Miyamoto M, Ishikawa T.
Bioorg Med Chem Lett (2016) 26 : 4296 -4300
PubMed 27476141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.26 7.41
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468555 2 7.41
CHEMBL4515745 2 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468555 EC50 = 39.0 nM 7.41
CHEMBL4515745 EC50 = 79.0 nM 7.10
CHEMBL4515745 Inhibition - % -
CHEMBL4468555 Inhibition - % -