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Assay Detail

CHEMBL4029702

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

Binding
Inhibition of recombinant human full length N-terminal GST-tagged PIM1 expressed in Escherichia coli using LKKRNRTLTV as substrate measured after 40 mins in presence of [gamma32P]ATP by scintillation counting method
1
Total Activities
1
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-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.
Bataille CJ, Brennan MB, Byrne S, Davies SG, Durbin M, Fedorov O, Huber KV, Jones AM, Knapp S, Liu G, Nadali A, Quevedo CE, Russell AJ, Walker RG, Westwood R, Wynne GM.
Bioorg Med Chem (2017) 25 : 2657 -2665
PubMed 28341403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1952329 SGI-1776 1.0 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1952329 SGI-1776 IC50 = 7.0 nM 8.15