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Assay Detail

CHEMBL908795

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

Functional
Inhibition of MCF7 cell proliferation (mean of two experiments)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Intermediate

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Price S, Bordogna W, Bull RJ, Clark DE, Crackett PH, Dyke HJ, Gill M, Harris NV, Gorski J, Lloyd J, Lockey PM, Mullett J, Roach AG, Roussel F, White AB.
Bioorg Med Chem Lett (2007) 17 : 370 -375
PubMed 17095213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.48 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217004 1 7.22
CHEMBL386473 1 7.22
CHEMBL218511 1 7.10
CHEMBL216249 1 7.00
CHEMBL426343 1 6.92
CHEMBL385406 1 6.92
CHEMBL216248 1 6.85
CHEMBL217186 1 6.85
CHEMBL385852 1 6.82
CHEMBL216625 1 6.77
CHEMBL217098 1 6.72
CHEMBL384961 1 6.70
CHEMBL217716 1 6.52
CHEMBL217468 1 6.46
CHEMBL386752 1 6.43
CHEMBL386135 1 6.34
CHEMBL216499 1 6.33
CHEMBL218514 1 6.30
CHEMBL218080 1 6.28
CHEMBL217029 1 6.10
CHEMBL216359 1 5.91
CHEMBL98 VORINOSTAT 4.0 1 5.82
CHEMBL217604 1 5.80
CHEMBL218236 1 5.69
CHEMBL216885 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217004 IC50 = 60.0 nM 7.22
CHEMBL386473 IC50 = 60.0 nM 7.22
CHEMBL218511 IC50 = 80.0 nM 7.10
CHEMBL216249 IC50 = 100.0 nM 7.00
CHEMBL426343 IC50 = 120.0 nM 6.92
CHEMBL385406 IC50 = 120.0 nM 6.92
CHEMBL216248 IC50 = 140.0 nM 6.85
CHEMBL217186 IC50 = 140.0 nM 6.85
CHEMBL385852 IC50 = 150.0 nM 6.82
CHEMBL216625 IC50 = 170.0 nM 6.77
CHEMBL217098 IC50 = 190.0 nM 6.72
CHEMBL384961 IC50 = 200.0 nM 6.70
CHEMBL217716 IC50 = 300.0 nM 6.52
CHEMBL217468 IC50 = 350.0 nM 6.46
CHEMBL386752 IC50 = 370.0 nM 6.43
CHEMBL386135 IC50 = 460.0 nM 6.34
CHEMBL216499 IC50 = 470.0 nM 6.33
CHEMBL218514 IC50 = 500.0 nM 6.30
CHEMBL218080 IC50 = 520.0 nM 6.28
CHEMBL217029 IC50 = 800.0 nM 6.10
CHEMBL216359 IC50 = 1240.0 nM 5.91
CHEMBL98 VORINOSTAT IC50 = 1500.0 nM 5.82
CHEMBL217604 IC50 = 1580.0 nM 5.80
CHEMBL218236 IC50 = 2060.0 nM 5.69
CHEMBL216885 IC50 = 11400.0 nM 4.94