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Assay Detail

CHEMBL908225

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Functional
Inhibition of HCT116 cell proliferation (mean of two experiments)
17
Total Activities
17
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 Intermediate

Target

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

Publication

Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Price S, Bordogna W, Braganza R, Bull RJ, Dyke HJ, Gardan S, Gill M, Harris NV, Heald RA, van den Heuvel M, Lockey PM, Lloyd J, Molina AG, Roach AG, Roussel F, Sutton JM, White AB.
Bioorg Med Chem Lett (2007) 17 : 363 -369
PubMed 17107790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.87 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216896 1 7.22
CHEMBL216463 1 7.16
CHEMBL441699 1 7.16
CHEMBL387447 1 7.10
CHEMBL385934 1 7.10
CHEMBL217882 1 7.05
CHEMBL436964 1 7.05
CHEMBL216301 1 7.00
CHEMBL216300 1 7.00
CHEMBL217615 1 6.96
CHEMBL216884 1 6.96
CHEMBL217246 1 6.92
CHEMBL384733 1 6.85
CHEMBL218392 1 6.75
CHEMBL385562 1 6.75
CHEMBL217716 1 6.24
CHEMBL98 VORINOSTAT 4.0 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216896 IC50 = 60.0 nM 7.22
CHEMBL216463 IC50 = 70.0 nM 7.16
CHEMBL441699 IC50 = 70.0 nM 7.16
CHEMBL387447 IC50 = 80.0 nM 7.10
CHEMBL385934 IC50 = 80.0 nM 7.10
CHEMBL217882 IC50 = 90.0 nM 7.05
CHEMBL436964 IC50 = 90.0 nM 7.05
CHEMBL216301 IC50 = 100.0 nM 7.00
CHEMBL216300 IC50 = 100.0 nM 7.00
CHEMBL217615 IC50 = 110.0 nM 6.96
CHEMBL216884 IC50 = 110.0 nM 6.96
CHEMBL217246 IC50 = 120.0 nM 6.92
CHEMBL384733 IC50 = 140.0 nM 6.85
CHEMBL218392 IC50 = 180.0 nM 6.75
CHEMBL385562 IC50 = 180.0 nM 6.75
CHEMBL217716 IC50 = 580.0 nM 6.24
CHEMBL98 VORINOSTAT IC50 = 2520.0 nM 5.60