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Assay Detail

CHEMBL4193845

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

Binding
Inhibition of full-length KDM4C (unknown origin) expressed in human KYSE-150 cells assessed as increase in H3K36me3 level after 24 hrs by Western blot analysis
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysine-specific demethylase 4C (CHEMBL6175)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models.
Chen YK, Bonaldi T, Cuomo A, Del Rosario JR, Hosfield DJ, Kanouni T, Kao SC, Lai C, Lobo NA, Matuszkiewicz J, McGeehan A, O'Connell SM, Shi L, Stafford JA, Stansfield RK, Veal JM, Weiss MS, Yuen NY, Wallace MB.
ACS Med Chem Lett (2017) 8 : 869 -874
PubMed 28835804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.59 8.89
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4216044 1 8.89
CHEMBL4216399 1 7.72
CHEMBL4207071 1 7.50
CHEMBL4211946 2 6.25
CHEMBL4202719 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4216044 EC50 = 1.3 nM 8.89
CHEMBL4216399 EC50 = 19.0 nM 7.72
CHEMBL4207071 EC50 = 32.0 nM 7.50
CHEMBL4211946 EC50 = 560.0 nM 6.25
CHEMBL4211946 Inhibition - % -
CHEMBL4202719 Inhibition - % -