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Compound Detail

CHEMBL4452281

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Cc1ccc(Nc2nccc(-c3c(-c4ccc(F)cc4)ncn3C3CCNCC3)n2)cc1C

Basic Information

ChEMBL ID CHEMBL4452281
Phase Preclinical
Structure Type MOL
InChI Key OGDBBVMMKPWVLG-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

442.5
MW (Da)
5.43
ALogP
6
HBA
2
HBD
67.7
PSA (Ų)
0.43
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27FN6
MW 442.54
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.35

Activity Summary

IC50 2 meas. best 5.89
Kd 1 meas. best 5.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.89 5.89 1300.0 1
Bromodomain-containing protein 4
CHEMBL1163125
Kd 5.75 5.75 1800.0 1
Bromodomain testis-specific protein
CHEMBL1795185
IC50 5.33 5.33 4700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30253095 10.1021/acs.jmedchem.8b01248 Bromodomain-containing protein 4 5
30253095 10.1021/acs.jmedchem.8b01248 Bromodomain testis-specific protein 3
30253095 10.1021/acs.jmedchem.8b01248 A549 1
30253095 10.1021/acs.jmedchem.8b01248 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine