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Assay Detail

CHEMBL4827616

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

Binding
Inhibition of NanoLuc-fused CAMKK2 (unknown origin) expressed in HEK293 cells after 24 hrs by NanoBRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 19 6.48 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870467 1 8.09
CHEMBL4852523 1 6.85
CHEMBL4862562 1 6.77
CHEMBL4877552 1 6.72
CHEMBL4851925 1 6.70
CHEMBL4875005 1 6.68
CHEMBL4869147 1 6.62
CHEMBL4876404 1 6.54
CHEMBL4873692 1 6.33
CHEMBL4851892 1 6.28
CHEMBL4877634 1 6.27
CHEMBL4866741 1 6.16
CHEMBL4849143 1 6.05
CHEMBL4857601 1 6.02
CHEMBL4853274 1 5.85
CHEMBL4878827 1 5.72
CHEMBL4125686 1 -
CHEMBL4857253 1 -
CHEMBL558642 GSK-650394 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870467 IC50 = 8.1 nM 8.09
CHEMBL4852523 IC50 = 140.0 nM 6.85
CHEMBL4862562 IC50 = 170.0 nM 6.77
CHEMBL4877552 IC50 = 190.0 nM 6.72
CHEMBL4851925 IC50 = 200.0 nM 6.70
CHEMBL4875005 IC50 = 210.0 nM 6.68
CHEMBL4869147 IC50 = 240.0 nM 6.62
CHEMBL4876404 IC50 = 290.0 nM 6.54
CHEMBL4873692 IC50 = 470.0 nM 6.33
CHEMBL4851892 IC50 = 530.0 nM 6.28
CHEMBL4877634 IC50 = 540.0 nM 6.27
CHEMBL4866741 IC50 = 700.0 nM 6.16
CHEMBL4849143 IC50 = 890.0 nM 6.05
CHEMBL4857601 IC50 = 950.0 nM 6.02
CHEMBL4853274 IC50 = 1400.0 nM 5.85
CHEMBL4878827 IC50 = 1900.0 nM 5.72
CHEMBL4125686 IC50 - -
CHEMBL4857253 IC50 < 3.0 nM -
CHEMBL558642 GSK-650394 IC50 < 3.0 nM -