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Assay Detail

CHEMBL5328197

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

Binding
Inhibition of SIK1 (unknown origin) using AMARA as substrate buffer incubated for 60 mins followed by addition of ADP-Glo reagent further incubated for 60 mins
12
Total Activities
12
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 SIK1 (CHEMBL6082)
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 12 7.23 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5405960 1 8.14
CHEMBL5426204 1 7.77
CHEMBL5430450 1 7.66
CHEMBL5394880 1 7.48
CHEMBL5415835 1 7.19
CHEMBL5407084 1 7.10
CHEMBL5421558 1 7.06
CHEMBL5415567 1 6.94
CHEMBL5434195 1 6.73
CHEMBL5393771 1 6.23
CHEMBL5428308 1 -
CHEMBL5420653 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5405960 IC50 = 7.3 nM 8.14
CHEMBL5426204 IC50 = 17.0 nM 7.77
CHEMBL5430450 IC50 = 22.0 nM 7.66
CHEMBL5394880 IC50 = 33.0 nM 7.48
CHEMBL5415835 IC50 = 65.0 nM 7.19
CHEMBL5407084 IC50 = 79.0 nM 7.10
CHEMBL5421558 IC50 = 88.0 nM 7.06
CHEMBL5415567 IC50 = 114.0 nM 6.94
CHEMBL5434195 IC50 = 188.0 nM 6.73
CHEMBL5393771 IC50 = 591.0 nM 6.23
CHEMBL5428308 IC50 - -
CHEMBL5420653 IC50 - -