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Assay Detail

CHEMBL4677637

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

Binding
Inhibition of ULK2 (unknown origin) expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase ULK2 (CHEMBL5435)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Ren H,Bakas NA,Vamos M,Chaikuad A,Limpert AS,Wimer CD,Brun SN,Lambert LJ,Tautz L,Celeridad M,Sheffler DJ,Knapp S,Shaw RJ,Cosford NDP
J Med Chem (2020) 63 : 14609 -14625
PubMed 33200929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.72 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741912 1 6.15
CHEMBL4779423 1 5.94
CHEMBL4746440 1 5.78
CHEMBL4789210 1 5.77
CHEMBL4795918 1 5.72
CHEMBL4800057 1 5.37
CHEMBL4128069 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741912 IC50 = 703.0 nM 6.15
CHEMBL4779423 IC50 = 1158.0 nM 5.94
CHEMBL4746440 IC50 = 1647.0 nM 5.78
CHEMBL4789210 IC50 = 1687.0 nM 5.77
CHEMBL4795918 IC50 = 1885.0 nM 5.72
CHEMBL4800057 IC50 = 4256.0 nM 5.37
CHEMBL4128069 IC50 = 4578.0 nM 5.34