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Assay Detail

CHEMBL5328196

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

Binding
Inhibition of SIK2 (unknown origin) using AMARA as substrate buffer incubated for 60 mins followed by addition of ADP-Glo reagent further incubated for 60 mins
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase SIK2 (CHEMBL5699)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel and selective SIK2 inhibitors by the application of AlphaFold structures and generative models.
Zhu W, Liu X, Li Q, Gao F, Liu T, Chen X, Zhang M, Aliper A, Ren F, Ding X, Zhavoronkov A.
Bioorg Med Chem (2023) 91 : 117414 -117414
PubMed 37467565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.49 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5394880 1 9.22
CHEMBL5430450 1 9.21
CHEMBL5426204 1 9.19
CHEMBL5421558 1 8.72
CHEMBL5405960 1 8.64
CHEMBL5420653 1 8.28
CHEMBL5415835 1 8.19
CHEMBL5407084 1 8.18
CHEMBL5415567 1 8.11
CHEMBL5434195 1 7.82
CHEMBL5393771 1 7.69
CHEMBL5434893 1 7.64
CHEMBL5436223 1 6.85
CHEMBL5428150 1 6.82
CHEMBL5435024 1 5.70
CHEMBL5433420 1 5.70
CHEMBL5437587 1 5.68
CHEMBL5399180 1 5.60
CHEMBL5408840 1 5.01
CHEMBL5428308 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5394880 IC50 = 0.6 nM 9.22
CHEMBL5430450 IC50 = 0.61 nM 9.21
CHEMBL5426204 IC50 = 0.64 nM 9.19
CHEMBL5421558 IC50 = 1.9 nM 8.72
CHEMBL5405960 IC50 = 2.3 nM 8.64
CHEMBL5420653 IC50 = 5.3 nM 8.28
CHEMBL5415835 IC50 = 6.4 nM 8.19
CHEMBL5407084 IC50 = 6.6 nM 8.18
CHEMBL5415567 IC50 = 7.8 nM 8.11
CHEMBL5434195 IC50 = 15.0 nM 7.82
CHEMBL5393771 IC50 = 20.4 nM 7.69
CHEMBL5434893 IC50 = 23.0 nM 7.64
CHEMBL5436223 IC50 = 140.0 nM 6.85
CHEMBL5428150 IC50 = 150.0 nM 6.82
CHEMBL5435024 IC50 = 2015.0 nM 5.70
CHEMBL5433420 IC50 = 2000.0 nM 5.70
CHEMBL5437587 IC50 = 2100.0 nM 5.68
CHEMBL5399180 IC50 = 2500.0 nM 5.60
CHEMBL5408840 IC50 = 9800.0 nM 5.01
CHEMBL5428308 IC50 > 10000.0 nM -