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Assay Detail

CHEMBL2019652

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

Functional
Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562
Confidence 1 — Organism
Curated By Autocuration

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of NAE Inhibitors Exhibiting Potent Activity in Leukemia Cells: Exploring the Structural Determinants of NAE Specificity.
Lukkarila JL, da Silva SR, Ali M, Shahani VM, Xu GW, Berman J, Roughton A, Dhe-Paganon S, Schimmer AD, Gunning PT.
ACS Med Chem Lett (2011) 2 : 577 -582
PubMed 24900352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.66 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231160 PEVONEDISTAT 3.0 1 6.97
CHEMBL2017016 1 6.94
CHEMBL2017005 1 6.90
CHEMBL2017008 1 6.88
CHEMBL2017007 1 6.80
CHEMBL2017006 1 6.74
CHEMBL2017012 1 6.69
CHEMBL2017018 1 6.42
CHEMBL2017017 1 6.25
CHEMBL2017009 1 6.03
CHEMBL2017011 1 -
CHEMBL2017010 1 -
CHEMBL2017013 1 -
CHEMBL2017014 1 -
CHEMBL2017015 1 -
CHEMBL2017019 1 -
CHEMBL2017020 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231160 PEVONEDISTAT EC50 = 108.0 nM 6.97
CHEMBL2017016 EC50 = 114.0 nM 6.94
CHEMBL2017005 EC50 = 125.0 nM 6.90
CHEMBL2017008 EC50 = 132.0 nM 6.88
CHEMBL2017007 EC50 = 160.0 nM 6.80
CHEMBL2017006 EC50 = 181.0 nM 6.74
CHEMBL2017012 EC50 = 203.0 nM 6.69
CHEMBL2017018 EC50 = 380.0 nM 6.42
CHEMBL2017017 EC50 = 559.0 nM 6.25
CHEMBL2017009 EC50 = 929.0 nM 6.03
CHEMBL2017011 EC50 > 1000.0 nM -
CHEMBL2017010 EC50 > 1000.0 nM -
CHEMBL2017013 EC50 > 1000.0 nM -
CHEMBL2017014 EC50 > 1000.0 nM -
CHEMBL2017015 EC50 > 1000.0 nM -
CHEMBL2017019 EC50 > 1000.0 nM -
CHEMBL2017020 EC50 > 1000.0 nM -