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Assay Detail

CHEMBL4222695

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

Binding
Inhibition of PIM2 (unknown origin) expressed in human U2OS cells assessed as reduction in BAD substrate phosphorylation by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase pim-2 (CHEMBL4523)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Gingipalli L, Block MH, Bao L, Cooke E, Dakin LA, Denz CR, Ferguson AD, Johannes JW, Larsen NA, Lyne PD, Pontz TW, Wang T, Wu X, Wu A, Zhang HJ, Zheng X, Dowling JE, Lamb ML.
Bioorg Med Chem Lett (2018) 28 : 1336 -1341
PubMed 29559278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.19 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4229130 1 5.72
CHEMBL4227817 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4229130 IC50 = 1900.0 nM 5.72
CHEMBL4227817 IC50 = 22000.0 nM 4.66