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Assay Detail

CHEMBL5355887

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

Binding
Inhibition of human recombinant HDAC1 using fluorogenic p53 (379-382 residues) (RHKK(Ac)AMC) as substrate
25
Total Activities
25
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

Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells.
Di Bello E, Sian V, Bontempi G, Zwergel C, Fioravanti R, Noce B, Castiello C, Tomassi S, Corinti D, Passeri D, Pellicciari R, Mercurio C, Varasi M, Altucci L, Tripodi M, Strippoli R, Nebbioso A, Valente S, Mai A.
Eur J Med Chem (2023) 247 : 115022 -115022
PubMed 36549114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.45 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5409409 1 7.20
CHEMBL5429873 1 7.17
CHEMBL5408688 1 7.11
CHEMBL98 VORINOSTAT 4.0 1 7.11
CHEMBL5400896 1 7.09
CHEMBL4550522 1 7.01
CHEMBL5396543 1 6.97
CHEMBL5429446 1 6.89
CHEMBL5412379 1 6.84
CHEMBL5396691 1 6.82
CHEMBL5417858 1 6.72
CHEMBL5419832 1 6.70
CHEMBL5414244 1 6.69
CHEMBL5433683 1 6.49
CHEMBL5399910 1 6.48
CHEMBL5409567 1 6.45
CHEMBL5401106 1 6.42
CHEMBL5420814 1 6.30
CHEMBL5411948 1 6.11
CHEMBL5425559 1 6.00
CHEMBL3426804 1 5.85
CHEMBL5418060 1 5.83
CHEMBL4521590 1 5.54
CHEMBL4435005 1 5.52
CHEMBL5426896 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5409409 IC50 = 63.0 nM 7.20
CHEMBL5429873 IC50 = 68.0 nM 7.17
CHEMBL5408688 IC50 = 77.0 nM 7.11
CHEMBL98 VORINOSTAT IC50 = 77.0 nM 7.11
CHEMBL5400896 IC50 = 81.0 nM 7.09
CHEMBL4550522 IC50 = 98.0 nM 7.01
CHEMBL5396543 IC50 = 108.0 nM 6.97
CHEMBL5429446 IC50 = 129.0 nM 6.89
CHEMBL5412379 IC50 = 143.0 nM 6.84
CHEMBL5396691 IC50 = 151.0 nM 6.82
CHEMBL5417858 IC50 = 189.0 nM 6.72
CHEMBL5419832 IC50 = 201.0 nM 6.70
CHEMBL5414244 IC50 = 203.0 nM 6.69
CHEMBL5433683 IC50 = 321.0 nM 6.49
CHEMBL5399910 IC50 = 330.0 nM 6.48
CHEMBL5409567 IC50 = 353.0 nM 6.45
CHEMBL5401106 IC50 = 376.0 nM 6.42
CHEMBL5420814 IC50 = 496.0 nM 6.30
CHEMBL5411948 IC50 = 783.0 nM 6.11
CHEMBL5425559 IC50 = 1010.0 nM 6.00
CHEMBL3426804 IC50 = 1420.0 nM 5.85
CHEMBL5418060 IC50 = 1490.0 nM 5.83
CHEMBL4521590 IC50 = 2850.0 nM 5.54
CHEMBL4435005 IC50 = 3000.0 nM 5.52
CHEMBL5426896 IC50 = 94000.0 nM 4.03