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Assay Detail

CHEMBL4394702

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

Binding
Inhibition of PIM3 (unknown origin) incubated for 60 mins using biotin-labelled STK substrate-1 as substrate by HTRF assay
2
Total Activities
2
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 pim-3 (CHEMBL5407)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Tong L, Song P, Jiang K, Xu L, Jin T, Wang P, Hu X, Fang S, Gao A, Zhou Y, Liu T, Li J, Hu Y.
Eur J Med Chem (2019) 173 : 44 -62
PubMed 30986571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.13 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4577258 1 6.13
CHEMBL3544911 PREXASERTIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4577258 IC50 = 735.53 nM 6.13
CHEMBL3544911 PREXASERTIB IC50 > 10000.0 nM -