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Assay Detail

CHEMBL908226

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

Functional
Inhibition of MDA-MB-231 cell proliferation (mean of two experiments)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Intermediate

Target

MDA-MB-231 (CHEMBL400)
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 14 6.19 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386914 1 6.77
CHEMBL217531 1 6.70
CHEMBL217097 1 6.68
CHEMBL216884 1 6.66
CHEMBL217529 1 6.60
CHEMBL387247 1 6.52
CHEMBL217881 1 6.52
CHEMBL217093 1 6.43
CHEMBL263570 1 6.20
CHEMBL217716 1 6.20
CHEMBL387105 1 6.07
CHEMBL425971 1 5.46
CHEMBL216509 1 4.96
CHEMBL98 VORINOSTAT 4.0 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386914 IC50 = 170.0 nM 6.77
CHEMBL217531 IC50 = 200.0 nM 6.70
CHEMBL217097 IC50 = 210.0 nM 6.68
CHEMBL216884 IC50 = 220.0 nM 6.66
CHEMBL217529 IC50 = 250.0 nM 6.60
CHEMBL387247 IC50 = 300.0 nM 6.52
CHEMBL217881 IC50 = 300.0 nM 6.52
CHEMBL217093 IC50 = 370.0 nM 6.43
CHEMBL263570 IC50 = 630.0 nM 6.20
CHEMBL217716 IC50 = 630.0 nM 6.20
CHEMBL387105 IC50 = 860.0 nM 6.07
CHEMBL425971 IC50 = 3510.0 nM 5.46
CHEMBL216509 IC50 = 11000.0 nM 4.96
CHEMBL98 VORINOSTAT IC50 = 12300.0 nM 4.91