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Assay Detail

CHEMBL5709115

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

Binding
Inhibition of GST-tagged NUAK1 (unknown origin) expressed in HEK293 cells using ALNRTSSDSALHRRR as substrate incubated for 30 mins in presence of [gamma-32P]-ATP by Cerenkov counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NUAK family SNF1-like kinase 1 (CHEMBL5784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS.
Biochem J (2014) 457 : 215 -225
PubMed 24171924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.76 8.82

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5303523 1 8.82
CHEMBL4303523 1 7.70
CHEMBL5190521 1 7.52
CHEMBL4303250 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5303523 IC50 = 1.5 nM 8.82
CHEMBL4303523 IC50 = 20.0 nM 7.70
CHEMBL5190521 IC50 = 30.0 nM 7.52
CHEMBL4303250 IC50 = 100.0 nM 7.00