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Assay Detail

CHEMBL4155089

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

Binding
Inhibition of recombinant human Pim1 expressed in bacterial expression system using histone H1 as substrate after 30 mins by ADP-Glo reagent based luminescence assay
18
Total Activities
18
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

Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.
Oyallon B, Brachet-Botineau M, Logé C, Bonnet P, Souab M, Robert T, Ruchaud S, Bach S, Berthelot P, Gouilleux F, Viaud-Massuard MC, Denevault-Sabourin C.
Eur J Med Chem (2018) 154 : 101 -109
PubMed 29778892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.48 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.51
CHEMBL4177432 1 7.13
CHEMBL4163110 1 6.54
CHEMBL4166554 1 6.12
CHEMBL4170635 1 6.00
CHEMBL4174068 1 5.55
CHEMBL4166150 1 -
CHEMBL4169579 1 -
CHEMBL4177174 1 -
CHEMBL4170051 1 -
CHEMBL4162053 1 -
CHEMBL4159749 1 -
CHEMBL4170384 1 -
CHEMBL4168687 1 -
CHEMBL4173649 1 -
CHEMBL4168098 1 -
CHEMBL4175950 1 -
CHEMBL4162709 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 31.0 nM 7.51
CHEMBL4177432 IC50 = 74.0 nM 7.13
CHEMBL4163110 IC50 = 290.0 nM 6.54
CHEMBL4166554 IC50 = 760.0 nM 6.12
CHEMBL4170635 IC50 = 1010.0 nM 6.00
CHEMBL4174068 IC50 = 2800.0 nM 5.55
CHEMBL4166150 IC50 > 10000.0 nM -
CHEMBL4169579 IC50 > 10000.0 nM -
CHEMBL4177174 IC50 > 10000.0 nM -
CHEMBL4170051 IC50 > 10000.0 nM -
CHEMBL4162053 IC50 > 10000.0 nM -
CHEMBL4159749 IC50 > 10000.0 nM -
CHEMBL4170384 IC50 > 10000.0 nM -
CHEMBL4168687 IC50 > 10000.0 nM -
CHEMBL4173649 IC50 > 10000.0 nM -
CHEMBL4168098 IC50 > 10000.0 nM -
CHEMBL4175950 IC50 > 10000.0 nM -
CHEMBL4162709 IC50 > 10000.0 nM -