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Compound Detail

CHEMBL4453121

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O=C(NO)c1ccc(Cn2nnc(-c3ncccn3)n2)cc1

Basic Information

ChEMBL ID CHEMBL4453121
Phase Preclinical
Structure Type MOL
InChI Key PMHARNDBRDSPAO-UHFFFAOYSA-N
11
Targets
12
Activities
1
Assay Types
0
PK Parameters
17
Publications
0
Known Names

Molecular Properties

297.3
MW (Da)
0.30
ALogP
8
HBA
2
HBD
118.7
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H11N7O2
MW 297.28
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.96

Activity Summary

IC50 12 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 8.15 8.15 7.0 2
Histone deacetylase 8
CHEMBL3192
IC50 6.5 6.5 320.0 1
Polyamine deacetylase HDAC10
CHEMBL5103
IC50 6.32 6.32 474.0 1
Histone deacetylase 11
CHEMBL3310
IC50 6.12 6.12 762.0 1
Histone deacetylase 3
CHEMBL1829
IC50 6.05 6.05 884.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.03 6.03 930.0 1
Histone deacetylase 7
CHEMBL2716
IC50 6.0 6.0 1010.0 1
Histone deacetylase 9
CHEMBL4145
IC50 5.77 5.77 1705.0 1
Histone deacetylase 2
CHEMBL1937
IC50 5.52 5.52 3007.0 1
Histone deacetylase 4
CHEMBL3524
IC50 5.34 5.34 4601.0 1
Histone deacetylase 5
CHEMBL2563
IC50 5.3 5.3 4999.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 6 IC50 = 7.0 nM 8.15 Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expresse... 31710483
Histone deacetylase 6 IC50 = 7.0 nM 8.15 Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expresse... 34795871
Histone deacetylase 8 IC50 = 320.0 nM 6.5 Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expresse... 34795871
Polyamine deacetylase HDAC10 IC50 = 474.0 nM 6.32 Inhibition of recombinant human N-terminal FLAG-tagged HDAC10 (1 to 613 residues... 34795871
Histone deacetylase 11 IC50 = 762.0 nM 6.12 Inhibition of recombinant human N-terminal His-tagged HDAC11 expressed in baculo... 34795871
Histone deacetylase 3 IC50 = 884.0 nM 6.05 Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 residues) ... 34795871
Histone deacetylase 1 IC50 = 930.0 nM 6.03 Inhibition of recombinant human C-terminal His-tagged HDAC1 expressed in Sf9 ins... 34795871
Histone deacetylase 7 IC50 = 1010.0 nM 6.0 Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues... 34795871
Histone deacetylase 9 IC50 = 1705.0 nM 5.77 Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residue... 34795871
Histone deacetylase 2 IC50 = 3007.0 nM 5.52 Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to 488 residues) ... 34795871
Histone deacetylase 4 IC50 = 4601.0 nM 5.34 Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged ... 34795871
Histone deacetylase 5 IC50 = 4999.0 nM 5.3 Inhibition of recombinant human ful length N-terminal GST-tagged HDAC5 expressed... 34795871

Literature References

Data from ChEMBL 36 via Core Engine