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Compound Detail

CHEMBL3394904

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COc1cc(/C=N/NC(=O)c2ccc(NC(=O)c3ccccn3)cc2)cc(Br)c1O

Basic Information

ChEMBL ID CHEMBL3394904
Phase Preclinical
Structure Type MOL
InChI Key XXUXBLAPIWSZSO-WYMPLXKRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

469.3
MW (Da)
3.57
ALogP
6
HBA
3
HBD
112.9
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17BrN4O4
MW 469.30
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.48

Activity Summary

IC50 1 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone chaperone ASF1A
CHEMBL3392950
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone chaperone ASF1A IC50 = 15000.0 nM 4.82 Inhibition of His-tagged human Asf1a binding with H3/H4 assessed as fluorescence... 25582598

Literature References

PubMed DOI Target Context # Activities
25582598 10.1016/j.bmcl.2014.11.067 Histone chaperone ASF1A 1

Data from ChEMBL 36 via Core Engine