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Compound Detail

CHEMBL4856110

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COc1cc2nc(-c3ccc(C)o3)cc(NCC3CCN(c4ncc(C(=O)NO)cn4)CC3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL4856110
Phase Preclinical
Structure Type MOL
InChI Key DDJFEVNAMKGVES-UHFFFAOYSA-N
7
Targets
10
Activities
1
Assay Types
8
PK Parameters
20
Publications
0
Known Names

Molecular Properties

518.6
MW (Da)
4.06
ALogP
10
HBA
3
HBD
134.9
PSA (Ų)
0.23
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N6O5
MW 518.57
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.12

Activity Summary

IC50 10 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 8.15 8.15 7.0 2
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2)
CHEMBL2111363
IC50 7.75 7.75 18.0 1
Histone deacetylase 2
CHEMBL1937
IC50 7.29 7.29 51.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.28 6.28 531.0 2
DNA (cytosine-5)-methyltransferase 3A
CHEMBL1992
IC50 5.75 5.75 1800.0 1
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.67 5.67 2160.0 2
DNA (cytosine-5)-methyltransferase 3B
CHEMBL6095
IC50 5.64 5.64 2300.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 306.53 ng.hr.mL-1 Mus musculus
AUC 475.11 ng.hr.mL-1 Mus musculus
CL 54.2 mL.min-1.kg-1 Homo sapiens
CL 410.7 mL.min-1.kg-1 Mus musculus
T1/2 1.185 hr Homo sapiens
T1/2 0.38 hr Mus musculus
T1/2 3.8 hr Mus musculus
T1/2 8.46 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33661013 10.1021/acs.jmedchem.0c02255 ADMET 16
33661013 10.1021/acs.jmedchem.0c02255 Unchecked 3
33661013 10.1021/acs.jmedchem.0c02255 MM1.S 3
33661013 10.1021/acs.jmedchem.0c02255 THLE-2 2
33661013 10.1021/acs.jmedchem.0c02255 Histone-lysine N-methyltransferase EHMT2 2
33661013 10.1021/acs.jmedchem.0c02255 Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) 1
33661013 10.1021/acs.jmedchem.0c02255 Histone deacetylase 6 1
33661013 10.1021/acs.jmedchem.0c02255 Histone deacetylase 2 1
33661013 10.1021/acs.jmedchem.0c02255 DNA (cytosine-5)-methyltransferase 1 1
33661013 10.1021/acs.jmedchem.0c02255 Histone deacetylase 1 1
33661013 10.1021/acs.jmedchem.0c02255 NCI-H929 1
33661013 10.1021/acs.jmedchem.0c02255 JJN-3 1
33661013 10.1021/acs.jmedchem.0c02255 Histone deacetylase 1
33661013 10.1021/acs.jmedchem.0c02255 Cytochrome P450 1A2 1
33661013 10.1021/acs.jmedchem.0c02255 Cytochrome P450 2C9 1
33661013 10.1021/acs.jmedchem.0c02255 Cytochrome P450 2C19 1
33661013 10.1021/acs.jmedchem.0c02255 Cytochrome P450 2D6 1
33661013 10.1021/acs.jmedchem.0c02255 Cytochrome P450 3A4 1
33661013 10.1021/acs.jmedchem.0c02255 No relevant target 1
39264152 10.1021/acs.jmedchem.4c01310 Histone deacetylase 1 1

Data from ChEMBL 36 via Core Engine