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Compound Detail

CHEMBL4078047

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COc1ccccc1C(=O)Nc1cc2cc(C)c(=O)n(C)c2cc1N1CCCC1

Basic Information

ChEMBL ID CHEMBL4078047
Phase Preclinical
Structure Type MOL
InChI Key COGXRBWRVXDPDM-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

391.5
MW (Da)
3.71
ALogP
5
HBA
1
HBD
63.6
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25N3O3
MW 391.47
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.18

Activity Summary

IC50 5 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peregrin
CHEMBL3132741
IC50 6.66 6.66 220.0 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 6.38 6.38 420.0 1
Bromodomain-containing protein 1
CHEMBL2176774
IC50 5.58 5.58 2600.0 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.34 5.34 4600.0 1
Bromodomain and PHD finger-containing protein 3
CHEMBL3108644
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28068087 10.1021/acs.jmedchem.6b01583 Unchecked 1
28068087 10.1021/acs.jmedchem.6b01583 Bromodomain-containing protein 4 1
28068087 10.1021/acs.jmedchem.6b01583 Bromodomain and PHD finger-containing protein 3 1
28068087 10.1021/acs.jmedchem.6b01583 Bromodomain-containing protein 1 1
28068087 10.1021/acs.jmedchem.6b01583 Bromodomain-containing protein 9 1
28068087 10.1021/acs.jmedchem.6b01583 Peregrin 1

Data from ChEMBL 36 via Core Engine