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Assay Detail

CHEMBL4373005

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Binding
Inhibition of human ERG
15
Total Activities
13
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

Publication

Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III.
Barberis C, Pribish J, Tserlin E, Gross A, Czekaj M, Barragué M, Erdman P, Maniar S, Jiang J, Fire L, Patel V, Hebert A, Levit M, Wang A, Sun F, Huang SA.
Bioorg Med Chem Lett (2019) 29 : 491 -495
PubMed 30553737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.49 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457529 1 8.96
CHEMBL4466764 1 8.85
CHEMBL4528544 1 8.77
CHEMBL4540910 1 8.52
CHEMBL4470576 1 8.52
CHEMBL4445116 1 8.52
CHEMBL4541837 1 8.40
CHEMBL4518492 2 8.30
CHEMBL4457389 1 8.30
CHEMBL4583118 2 8.22
CHEMBL4563802 1 -
CHEMBL4446498 1 -
CHEMBL4533366 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457529 IC50 = 1.1 nM 8.96
CHEMBL4466764 IC50 = 1.4 nM 8.85
CHEMBL4528544 IC50 = 1.7 nM 8.77
CHEMBL4540910 IC50 = 3.0 nM 8.52
CHEMBL4470576 IC50 = 3.0 nM 8.52
CHEMBL4445116 IC50 = 3.0 nM 8.52
CHEMBL4541837 IC50 = 4.0 nM 8.40
CHEMBL4518492 IC50 = 5.0 nM 8.30
CHEMBL4457389 IC50 = 5.0 nM 8.30
CHEMBL4583118 IC50 = 6.0 nM 8.22
CHEMBL4518492 IC50 = 10.0 nM 8.00
CHEMBL4563802 IC50 > 20.0 nM -
CHEMBL4446498 IC50 > 20.0 nM -
CHEMBL4533366 IC50 > 10.0 nM -
CHEMBL4583118 IC50 > 20.0 nM -