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Assay Detail

CHEMBL5318939

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

Binding
Inhibition of human full length-His6 tagged PIM1 (1 to 312 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using RSRHSSYPAGT as peptide substrate incubated for 10 mins in presence of [gamma-32P]ATP by radiometric scintillation assay
4
Total Activities
4
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

Targeting Death-Associated Protein Kinases for Treatment of Human Diseases: Recent Advances and Future Directions.
Zhang L, Luo B, Lu Y, Chen Y.
J Med Chem (2023) 66 : 1112 -1136
PubMed 36645394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.44 5.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425555 1 5.83
CHEMBL5303531 1 5.53
CHEMBL5413882 1 5.20
CHEMBL5410656 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425555 Ki = 1480.0 nM 5.83
CHEMBL5303531 Ki = 2940.0 nM 5.53
CHEMBL5413882 Ki = 6310.0 nM 5.20
CHEMBL5410656 Ki = 6480.0 nM 5.19