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Assay Detail

CHEMBL3240086

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Functional
Inhibition of human HCT116 cell growth
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Kawamura S, Unno Y, Asai A, Arisawa M, Shuto S.
J Med Chem (2014) 57 : 2726 -2735
PubMed 24524217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.01 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 8.30
CHEMBL3237863 1 7.50
CHEMBL3237864 1 7.37
CHEMBL3237870 1 7.35
CHEMBL3237862 1 7.34
CHEMBL3237869 1 7.22
CHEMBL3237865 1 7.20
CHEMBL3237867 1 7.17
CHEMBL3237874 1 7.10
CHEMBL3237866 1 6.96
CHEMBL3237873 1 6.89
CHEMBL3237868 1 6.85
CHEMBL3237871 1 6.58
CHEMBL3237860 1 5.74
CHEMBL3237872 1 5.60
CHEMBL3237861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 5.0 nM 8.30
CHEMBL3237863 IC50 = 31.8 nM 7.50
CHEMBL3237864 IC50 = 43.0 nM 7.37
CHEMBL3237870 IC50 = 45.0 nM 7.35
CHEMBL3237862 IC50 = 45.4 nM 7.34
CHEMBL3237869 IC50 = 60.0 nM 7.22
CHEMBL3237865 IC50 = 63.6 nM 7.20
CHEMBL3237867 IC50 = 67.2 nM 7.17
CHEMBL3237874 IC50 = 79.6 nM 7.10
CHEMBL3237866 IC50 = 110.3 nM 6.96
CHEMBL3237873 IC50 = 130.0 nM 6.89
CHEMBL3237868 IC50 = 140.0 nM 6.85
CHEMBL3237871 IC50 = 260.0 nM 6.58
CHEMBL3237860 IC50 = 1820.0 nM 5.74
CHEMBL3237872 IC50 = 2500.0 nM 5.60
CHEMBL3237861 IC50 > 10000.0 nM -