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Assay Detail

CHEMBL4827620

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

Binding
Inhibition of CAMKK2 in human LNCaP C4-2 cells assessed as reduction AMPK phosphorylation at Thr172 incubated for 24 hrs by Western blot analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LNCaP C4-2
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

Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes.
Eduful BJ, O'Byrne SN, Temme L, Asquith CRM, Liang Y, Picado A, Pilotte JR, Hossain MA, Wells CI, Zuercher WJ, Catta-Preta CMC, Zonzini Ramos P, Santiago AS, Couñago RM, Langendorf CG, Nay K, Oakhill JS, Pulliam TL, Lin C, Awad D, Willson TM, Frigo DE, Scott JW, Drewry DH.
J Med Chem (2021) 64 : 10849 -10877
PubMed 34264658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.81 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852523 1 6.41
CHEMBL4876404 1 6.10
CHEMBL4877552 1 6.05
CHEMBL4869147 1 6.01
CHEMBL4870467 1 5.75
CHEMBL4125686 1 5.26
CHEMBL4862562 1 5.09
CHEMBL4857253 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852523 IC50 = 390.0 nM 6.41
CHEMBL4876404 IC50 = 790.0 nM 6.10
CHEMBL4877552 IC50 = 900.0 nM 6.05
CHEMBL4869147 IC50 = 980.0 nM 6.01
CHEMBL4870467 IC50 = 1800.0 nM 5.75
CHEMBL4125686 IC50 = 5500.0 nM 5.26
CHEMBL4862562 IC50 = 8100.0 nM 5.09
CHEMBL4857253 IC50 < 39.0 nM -