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Assay Detail

CHEMBL5377229

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

Binding
Induction of ePL tagged degradation of CaMKK2 (unknown origin) expressed in HEK292T cells incubated for 24 hrs by luminescence based analysis
9
Total Activities
9
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

Calcium/calmodulin-dependent protein kinase kinase 2 (CHEMBL5284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2).
Chen Y, Whitefield B, Nevius E, Hill M, DelRosario J, Sinitsyna N, Shanmugasundaram V, Mukherjee D, Shi L, Mayne CG, Rousseau AM, Bernard SM, Buenviaje J, Khambatta G, El Samin M, Wallace M, Nie Z, Sivakumar P, Hamann LG, McDonnell DP, D'Agostino LA.
J Med Chem (2023) 66 : 15750 -15760
PubMed 38009718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.06 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422255 1 6.54
CHEMBL5394508 1 6.29
CHEMBL5416036 1 6.28
CHEMBL5412289 1 6.21
CHEMBL5395520 1 5.70
CHEMBL5434028 1 5.35
CHEMBL5430196 1 -
CHEMBL5440885 1 -
CHEMBL5424004 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422255 EC50 = 290.0 nM 6.54
CHEMBL5394508 EC50 = 510.0 nM 6.29
CHEMBL5416036 EC50 = 530.0 nM 6.28
CHEMBL5412289 EC50 = 620.0 nM 6.21
CHEMBL5395520 EC50 = 2000.0 nM 5.70
CHEMBL5434028 EC50 = 4500.0 nM 5.35
CHEMBL5430196 EC50 > 10000.0 nM -
CHEMBL5440885 EC50 > 10000.0 nM -
CHEMBL5424004 EC50 > 10000.0 nM -