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Assay Detail

CHEMBL5709117

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

Binding
Inhibition of GST-tagged NUAK1 A195T (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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5.83 6.22

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 6.22
CHEMBL4303523 1 6.05
CHEMBL5190521 1 5.82
CHEMBL4303250 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5303523 IC50 = 600.0 nM 6.22
CHEMBL4303523 IC50 = 900.0 nM 6.05
CHEMBL5190521 IC50 = 1500.0 nM 5.82
CHEMBL4303250 IC50 = 5888.0 nM 5.23