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Assay Detail

CHEMBL5608263

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

Binding
Inhibition of Nano Luc-fused PIM3 (unknown origin) expressed in HEK293 cells using NanoGlo as substrate by NanoBRET In-cell target engagement assay
23
Total Activities
23
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

Serine/threonine-protein kinase pim-3 (CHEMBL5407)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.
Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM.
Bioorg Med Chem Lett (2024) 99 : 129617 -129617
PubMed 38199328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.02 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5613918 1 7.96
CHEMBL5613782 1 7.96
CHEMBL4228654 1 7.75
CHEMBL5614352 1 7.70
CHEMBL5613647 1 7.70
CHEMBL4224859 1 7.55
CHEMBL5612624 1 7.52
CHEMBL5613324 1 7.21
CHEMBL5614031 1 7.18
CHEMBL4225287 1 6.64
CHEMBL5612131 1 6.62
CHEMBL5612824 1 6.47
CHEMBL5612698 1 6.38
CHEMBL5612145 1 6.37
CHEMBL5613954 1 5.70
CHEMBL5612629 1 5.62
CHEMBL5613392 1 -
CHEMBL5614321 1 -
CHEMBL5613700 1 -
CHEMBL5612961 1 -
CHEMBL5612856 1 -
CHEMBL5613798 1 -
CHEMBL5611959 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5613918 IC50 = 11.0 nM 7.96
CHEMBL5613782 IC50 = 11.0 nM 7.96
CHEMBL4228654 IC50 = 18.0 nM 7.75
CHEMBL5614352 IC50 = 20.0 nM 7.70
CHEMBL5613647 IC50 = 20.0 nM 7.70
CHEMBL4224859 IC50 = 28.0 nM 7.55
CHEMBL5612624 IC50 = 30.0 nM 7.52
CHEMBL5613324 IC50 = 61.0 nM 7.21
CHEMBL5614031 IC50 = 66.0 nM 7.18
CHEMBL4225287 IC50 = 230.0 nM 6.64
CHEMBL5612131 IC50 = 240.0 nM 6.62
CHEMBL5612824 IC50 = 340.0 nM 6.47
CHEMBL5612698 IC50 = 420.0 nM 6.38
CHEMBL5612145 IC50 = 430.0 nM 6.37
CHEMBL5613954 IC50 = 2000.0 nM 5.70
CHEMBL5612629 IC50 = 2400.0 nM 5.62
CHEMBL5613392 IC50 - -
CHEMBL5614321 IC50 - -
CHEMBL5613700 IC50 - -
CHEMBL5612961 IC50 - -
CHEMBL5612856 IC50 - -
CHEMBL5613798 IC50 - -
CHEMBL5611959 IC50 - -