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Assay Detail

CHEMBL907072

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

Binding
Inhibition of HDAC1 (mean IC50)
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A series of novel, potent, and selective histone deacetylase inhibitors.
Jones P, Altamura S, Chakravarty PK, Cecchetti O, De Francesco R, Gallinari P, Ingenito R, Meinke PT, Petrocchi A, Rowley M, Scarpelli R, Serafini S, Steinkühler C.
Bioorg Med Chem Lett (2006) 16 : 5948 -5952
PubMed 16987657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.83 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216641 1 9.10
CHEMBL386069 1 7.75
CHEMBL384804 1 7.64
CHEMBL217509 1 7.60
CHEMBL98 VORINOSTAT 4.0 1 7.57
CHEMBL217781 1 7.48
CHEMBL430060 APICIDIN 1 7.36
CHEMBL216176 1 7.36
CHEMBL217651 1 7.26
CHEMBL217650 1 7.26
CHEMBL217314 1 7.10
CHEMBL385238 1 7.00
CHEMBL27759 ENTINOSTAT 3.0 1 6.96
CHEMBL385550 1 6.82
CHEMBL384993 1 6.75
CHEMBL217371 1 6.72
CHEMBL387224 1 6.70
CHEMBL387015 1 6.66
CHEMBL384384 1 6.66
CHEMBL216427 1 6.64
CHEMBL384463 1 6.46
CHEMBL425629 1 6.32
CHEMBL218129 1 6.27
CHEMBL385626 1 6.25
CHEMBL412598 1 6.23
CHEMBL217035 1 6.23
CHEMBL216336 1 6.03
CHEMBL217025 1 5.75
CHEMBL384472 1 5.50
CHEMBL216414 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216641 IC50 = 0.8 nM 9.10
CHEMBL386069 IC50 = 18.0 nM 7.75
CHEMBL384804 IC50 = 23.0 nM 7.64
CHEMBL217509 IC50 = 25.0 nM 7.60
CHEMBL98 VORINOSTAT IC50 = 27.0 nM 7.57
CHEMBL217781 IC50 = 33.0 nM 7.48
CHEMBL430060 APICIDIN IC50 = 44.0 nM 7.36
CHEMBL216176 IC50 = 44.0 nM 7.36
CHEMBL217651 IC50 = 55.0 nM 7.26
CHEMBL217650 IC50 = 55.0 nM 7.26
CHEMBL217314 IC50 = 79.0 nM 7.10
CHEMBL385238 IC50 = 100.0 nM 7.00
CHEMBL27759 ENTINOSTAT IC50 = 110.0 nM 6.96
CHEMBL385550 IC50 = 150.0 nM 6.82
CHEMBL384993 IC50 = 180.0 nM 6.75
CHEMBL217371 IC50 = 190.0 nM 6.72
CHEMBL387224 IC50 = 200.0 nM 6.70
CHEMBL387015 IC50 = 220.0 nM 6.66
CHEMBL384384 IC50 = 220.0 nM 6.66
CHEMBL216427 IC50 = 230.0 nM 6.64
CHEMBL384463 IC50 = 350.0 nM 6.46
CHEMBL425629 IC50 = 480.0 nM 6.32
CHEMBL218129 IC50 = 540.0 nM 6.27
CHEMBL385626 IC50 = 560.0 nM 6.25
CHEMBL412598 IC50 = 590.0 nM 6.23
CHEMBL217035 IC50 = 590.0 nM 6.23
CHEMBL216336 IC50 = 930.0 nM 6.03
CHEMBL217025 IC50 = 1760.0 nM 5.75
CHEMBL384472 IC50 = 3200.0 nM 5.50
CHEMBL216414 IC50 = 3300.0 nM 5.48
CHEMBL386557 IC50 > 5000.0 nM -
CHEMBL412599 IC50 > 5000.0 nM -
CHEMBL386965 IC50 > 5000.0 nM -