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Assay Detail

CHEMBL4253403

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

Binding
Inhibition of recombinant human GST-tagged NIK expressed in baculovirus expression system using ser/thr-7 as substrate preincubated for 15 mins followed by ATP addition measured after 60 mins
1
Total Activities
1
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

Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H.
Eur J Med Chem (2018) 144 : 1 -28
PubMed 29247857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.35 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4277900 CROZBACICLIB 2.0 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4277900 CROZBACICLIB IC50 = 45.0 nM 7.35