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Assay Detail

CHEMBL4677634

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

Binding
Inhibition of ULK1 (unknown origin) expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay
26
Total Activities
26
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 ULK1 (CHEMBL6006)
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 26 5.84 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4779423 1 6.48
CHEMBL4795918 1 6.24
CHEMBL4741912 1 6.23
CHEMBL4789210 1 6.17
CHEMBL4746440 1 6.13
CHEMBL4128069 1 6.11
CHEMBL4800057 1 5.99
CHEMBL4782961 1 5.93
CHEMBL4750700 1 5.92
CHEMBL4778997 1 5.88
CHEMBL4796600 1 5.87
CHEMBL4748400 1 5.83
CHEMBL4794151 1 5.83
CHEMBL4787833 1 5.79
CHEMBL4758769 1 5.79
CHEMBL4786152 1 5.77
CHEMBL4776497 1 5.71
CHEMBL4747695 1 5.44
CHEMBL4799009 1 5.35
CHEMBL4755602 1 5.22
CHEMBL4754535 1 5.01
CHEMBL4793366 1 -
CHEMBL4792540 1 -
CHEMBL4777354 1 -
CHEMBL4748802 1 -
CHEMBL4794090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4779423 IC50 = 328.0 nM 6.48
CHEMBL4795918 IC50 = 582.0 nM 6.24
CHEMBL4741912 IC50 = 585.0 nM 6.23
CHEMBL4789210 IC50 = 679.0 nM 6.17
CHEMBL4746440 IC50 = 739.0 nM 6.13
CHEMBL4128069 IC50 = 785.0 nM 6.11
CHEMBL4800057 IC50 = 1021.0 nM 5.99
CHEMBL4782961 IC50 = 1168.0 nM 5.93
CHEMBL4750700 IC50 = 1215.0 nM 5.92
CHEMBL4778997 IC50 = 1327.0 nM 5.88
CHEMBL4796600 IC50 = 1361.0 nM 5.87
CHEMBL4748400 IC50 = 1464.0 nM 5.83
CHEMBL4794151 IC50 = 1477.0 nM 5.83
CHEMBL4787833 IC50 = 1611.0 nM 5.79
CHEMBL4758769 IC50 = 1602.0 nM 5.79
CHEMBL4786152 IC50 = 1713.0 nM 5.77
CHEMBL4776497 IC50 = 1926.0 nM 5.71
CHEMBL4747695 IC50 = 3631.0 nM 5.44
CHEMBL4799009 IC50 = 4475.0 nM 5.35
CHEMBL4755602 IC50 = 6038.0 nM 5.22
CHEMBL4754535 IC50 = 9838.0 nM 5.01
CHEMBL4793366 IC50 > 10000.0 nM -
CHEMBL4792540 IC50 > 10000.0 nM -
CHEMBL4777354 IC50 > 10000.0 nM -
CHEMBL4748802 IC50 > 10000.0 nM -
CHEMBL4794090 IC50 > 10000.0 nM -