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Assay Detail

CHEMBL3379478

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

Binding
Inhibition of HDAC1 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay
34
Total Activities
34
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

ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
Giannini G, Vesci L, Battistuzzi G, Vignola D, Milazzo FM, Guglielmi MB, Barbarino M, Santaniello M, Fantò N, Mor M, Rivara S, Pala D, Taddei M, Pisano C, Cabri W.
J Med Chem (2014) 57 : 8358 -8377
PubMed 25233084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.18 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356916 1 8.70
CHEMBL3356924 1 8.52
CHEMBL3356923 1 8.40
CHEMBL3356922 1 8.30
CHEMBL3353927 1 8.30
CHEMBL3356527 1 8.15
CHEMBL3356925 1 8.15
CHEMBL3356917 1 8.10
CHEMBL3356929 1 8.10
CHEMBL3356524 1 8.00
CHEMBL3356526 1 7.96
CHEMBL3356915 1 7.92
CHEMBL3356919 1 7.89
CHEMBL3356523 1 7.82
CHEMBL3356918 1 7.62
CHEMBL3356927 1 7.50
CHEMBL3356926 1 7.28
CHEMBL3356921 1 7.24
CHEMBL3356928 1 7.13
CHEMBL3356937 1 7.04
CHEMBL3356920 1 7.00
CHEMBL3356931 1 6.80
CHEMBL98 VORINOSTAT 4.0 1 6.59
CHEMBL325676 1 6.54
CHEMBL326433 8-MERCAPTO-OCTANOIC ACID PHENYLAMIDE 1 6.53
CHEMBL3356933 1 6.41
CHEMBL3356935 1 6.30
CHEMBL109654 1 6.10
CHEMBL3356930 1 6.06
CHEMBL3356938 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356916 IC50 = 2.0 nM 8.70
CHEMBL3356924 IC50 = 3.0 nM 8.52
CHEMBL3356923 IC50 = 4.0 nM 8.40
CHEMBL3356922 IC50 = 5.0 nM 8.30
CHEMBL3353927 IC50 = 5.0 nM 8.30
CHEMBL3356527 IC50 = 7.0 nM 8.15
CHEMBL3356925 IC50 = 7.0 nM 8.15
CHEMBL3356917 IC50 = 8.0 nM 8.10
CHEMBL3356929 IC50 = 8.0 nM 8.10
CHEMBL3356524 IC50 = 10.0 nM 8.00
CHEMBL3356526 IC50 = 11.0 nM 7.96
CHEMBL3356915 IC50 = 12.0 nM 7.92
CHEMBL3356919 IC50 = 13.0 nM 7.89
CHEMBL3356523 IC50 = 15.0 nM 7.82
CHEMBL3356918 IC50 = 24.0 nM 7.62
CHEMBL3356927 IC50 = 32.0 nM 7.50
CHEMBL3356926 IC50 = 53.0 nM 7.28
CHEMBL3356921 IC50 = 58.0 nM 7.24
CHEMBL3356928 IC50 = 74.0 nM 7.13
CHEMBL3356937 IC50 = 92.0 nM 7.04
CHEMBL3356920 IC50 = 101.0 nM 7.00
CHEMBL3356931 IC50 = 160.0 nM 6.80
CHEMBL98 VORINOSTAT IC50 = 258.0 nM 6.59
CHEMBL325676 IC50 = 288.0 nM 6.54
CHEMBL326433 8-MERCAPTO-OCTANOIC ACID PHENYLAMIDE IC50 = 294.0 nM 6.53
CHEMBL3356933 IC50 = 386.0 nM 6.41
CHEMBL3356935 IC50 = 504.0 nM 6.30
CHEMBL109654 IC50 = 791.0 nM 6.10
CHEMBL3356930 IC50 = 865.0 nM 6.06
CHEMBL3356938 IC50 = 1750.0 nM 5.76
CHEMBL3356939 IC50 = 2900.0 nM 5.54
CHEMBL3356934 IC50 = 3160.0 nM 5.50
CHEMBL3356936 IC50 = 3210.0 nM 5.49
CHEMBL3356932 IC50 = 5960.0 nM 5.22