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Compound Detail

CHEMBL410761

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Cn1nc(C(C)(C)C)cc1NC(=O)Nc1ccc(-c2ccc(CN3CCOCC3)nc2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL410761
Phase Preclinical
Structure Type MOL
InChI Key HTEMUDPCVAMLEB-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
5.41
ALogP
6
HBA
2
HBD
84.3
PSA (Ų)
0.38
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34N6O2
MW 498.63
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.75

Activity Summary

IC50 4 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
THP-1
CHEMBL614245
IC50 7.54 7.52 29.0 2
Blood
CHEMBL613416
IC50 6.64 6.33 230.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17560108 10.1016/j.bmcl.2007.05.042 THP-1 1
17560108 10.1016/j.bmcl.2007.05.042 Blood 1
17560108 10.1016/j.bmcl.2007.05.042 Mus musculus 1
19356929 10.1016/j.bmcl.2009.03.104 Blood 1
19356929 10.1016/j.bmcl.2009.03.104 THP-1 1
19356929 10.1016/j.bmcl.2009.03.104 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine