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Compound Detail

CHEMBL5087797

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Cc1ccc(C(C)C)cc1Oc1nccc(-c2c(-c3ccc(C(F)(F)F)cc3)ncn2C2CCN(CCN(C)C)CC2)n1

Basic Information

ChEMBL ID CHEMBL5087797
Phase Preclinical
Structure Type MOL
InChI Key CWBUVSFBCHVOPH-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

592.7
MW (Da)
7.45
ALogP
7
HBA
0
HBD
59.3
PSA (Ų)
0.20
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H39F3N6O
MW 592.71
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.20

Activity Summary

Kd 2 meas. best 7.82
EC50 1 meas. best 5.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 4
CHEMBL1163125
Kd 7.82 7.82 15.0 1
Mitogen-activated protein kinase 14
CHEMBL260
Kd 7.01 7.01 98.0 1
A549
CHEMBL392
EC50 5.44 5.44 3600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35007061 10.1021/acs.jmedchem.1c01779 Bromodomain-containing protein 4 5
35007061 10.1021/acs.jmedchem.1c01779 Unchecked 5
35007061 10.1021/acs.jmedchem.1c01779 Bromodomain-containing protein 2 4
35007061 10.1021/acs.jmedchem.1c01779 Bromodomain-containing protein 3 2
35007061 10.1021/acs.jmedchem.1c01779 A549 2
35007061 10.1021/acs.jmedchem.1c01779 Bromodomain testis-specific protein 1
35007061 10.1021/acs.jmedchem.1c01779 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine