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Compound Detail

CHEMBL429254

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Cc1ccccc1-n1nc(C(C)(C)C)cc1NC(=O)C(=O)c1ccc(OCCN2CCOCC2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL429254
Phase Preclinical
Structure Type MOL
InChI Key HKNRETMMTGULKN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

540.7
MW (Da)
5.16
ALogP
7
HBA
1
HBD
85.7
PSA (Ų)
0.25
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H36N4O4
MW 540.66
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
THP-1
CHEMBL614245
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
THP-1 IC50 = 1500.0 nM 5.82 Inhibition of LPS-induced TNFalpha production in human THP1 cells 18325768

Literature References

PubMed DOI Target Context # Activities
18325768 10.1016/j.bmcl.2008.02.033 THP-1 1

Data from ChEMBL 36 via Core Engine