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Assay Detail

CHEMBL960090

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

Binding
Inhibition of GST-tagged Pim2 after 15 mins by scintillation counting-based competition assay in presence of 1 uM [gamma33P]ATP
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Qian K, Wang L, Cywin CL, Farmer BT, Hickey E, Homon C, Jakes S, Kashem MA, Lee G, Leonard S, Li J, Magboo R, Mao W, Pack E, Peng C, Prokopowicz A, Welzel M, Wolak J, Morwick T.
J Med Chem (2009) 52 : 1814 -1827
PubMed 19256503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.85 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493937 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493937 IC50 = 140.0 nM 6.85