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Assay Detail

CHEMBL4222673

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

Binding
Inhibition of human PIM2
22
Total Activities
22
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-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 22 5.44 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4229130 1 6.85
CHEMBL4228654 1 5.85
CHEMBL4224859 1 5.55
CHEMBL4228363 1 5.16
CHEMBL4227817 1 5.07
CHEMBL4225287 1 5.00
CHEMBL4227886 1 4.58
CHEMBL4227556 1 -
CHEMBL4227028 1 -
CHEMBL4225330 1 -
CHEMBL4225224 1 -
CHEMBL4224959 1 -
CHEMBL4228394 1 -
CHEMBL4224693 1 -
CHEMBL4225206 1 -
CHEMBL4227791 1 -
CHEMBL4225896 1 -
CHEMBL4225046 1 -
CHEMBL4225633 1 -
CHEMBL4224786 1 -
CHEMBL4225378 1 -
CHEMBL4228564 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4229130 IC50 = 140.0 nM 6.85
CHEMBL4228654 IC50 = 1400.0 nM 5.85
CHEMBL4224859 IC50 = 2800.0 nM 5.55
CHEMBL4228363 IC50 = 6900.0 nM 5.16
CHEMBL4227817 IC50 = 8600.0 nM 5.07
CHEMBL4225287 IC50 = 10000.0 nM 5.00
CHEMBL4227886 IC50 = 26000.0 nM 4.58
CHEMBL4227556 IC50 > 30000.0 nM -
CHEMBL4227028 IC50 > 30000.0 nM -
CHEMBL4225330 IC50 > 30000.0 nM -
CHEMBL4225224 IC50 > 30000.0 nM -
CHEMBL4224959 IC50 > 30000.0 nM -
CHEMBL4228394 IC50 > 30000.0 nM -
CHEMBL4224693 IC50 > 30000.0 nM -
CHEMBL4225206 IC50 > 30000.0 nM -
CHEMBL4227791 IC50 > 30000.0 nM -
CHEMBL4225896 IC50 > 30000.0 nM -
CHEMBL4225046 IC50 > 30000.0 nM -
CHEMBL4225633 IC50 > 30000.0 nM -
CHEMBL4224786 IC50 > 30000.0 nM -
CHEMBL4225378 IC50 > 30000.0 nM -
CHEMBL4228564 IC50 > 30000.0 nM -