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Assay Detail

CHEMBL1832517

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Functional
Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET.
J Med Chem (2011) 54 : 4694 -4720
PubMed 21634430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.58 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489332 1 7.51
CHEMBL483254 PANOBINOSTAT 4.0 1 7.46
CHEMBL460963 1 6.96
CHEMBL1830540 1 6.85
CHEMBL491316 1 6.72
CHEMBL1830536 1 6.70
CHEMBL1830422 1 6.70
CHEMBL1830541 1 6.68
CHEMBL1830539 1 6.64
CHEMBL1830537 1 6.64
CHEMBL1830424 1 6.64
CHEMBL1830420 1 6.62
CHEMBL1830538 1 6.43
CHEMBL1830396 1 6.42
CHEMBL1830397 1 6.36
CHEMBL3215861 1 6.32
CHEMBL408513 BELINOSTAT 4.0 1 6.17
CHEMBL1830416 1 6.12
CHEMBL1828648 1 5.91
CHEMBL98 VORINOSTAT 4.0 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489332 IC50 = 31.0 nM 7.51
CHEMBL483254 PANOBINOSTAT IC50 = 35.0 nM 7.46
CHEMBL460963 IC50 = 110.0 nM 6.96
CHEMBL1830540 IC50 = 140.0 nM 6.85
CHEMBL491316 IC50 = 190.0 nM 6.72
CHEMBL1830536 IC50 = 200.0 nM 6.70
CHEMBL1830422 IC50 = 200.0 nM 6.70
CHEMBL1830541 IC50 = 210.0 nM 6.68
CHEMBL1830539 IC50 = 230.0 nM 6.64
CHEMBL1830537 IC50 = 230.0 nM 6.64
CHEMBL1830424 IC50 = 230.0 nM 6.64
CHEMBL1830420 IC50 = 240.0 nM 6.62
CHEMBL1830538 IC50 = 370.0 nM 6.43
CHEMBL1830396 IC50 = 380.0 nM 6.42
CHEMBL1830397 IC50 = 440.0 nM 6.36
CHEMBL3215861 IC50 = 480.0 nM 6.32
CHEMBL408513 BELINOSTAT IC50 = 670.0 nM 6.17
CHEMBL1830416 IC50 = 760.0 nM 6.12
CHEMBL1828648 IC50 = 1240.0 nM 5.91
CHEMBL98 VORINOSTAT IC50 = 1620.0 nM 5.79