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Compound Detail

CHEMBL516978

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Cc1cc(COc2ccc(N3CCC([C@H](NC(=O)OC(C)(C)C)C(=O)NO)C3=O)cc2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL516978
Phase Preclinical
Structure Type MOL
InChI Key LJHSZEIWFDSULF-GITCGBDTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
3.87
ALogP
7
HBA
3
HBD
130.1
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N4O6
MW 520.59
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 9.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Blood
CHEMBL613416
IC50 9.38 9.38 0.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Blood IC50 = 0.42 nM 9.38 Inhibition of TNFalpha production in human whole blood 19095454

Literature References

PubMed DOI Target Context # Activities
19095454 10.1016/j.bmc.2008.11.067 Unchecked 3
19095454 10.1016/j.bmc.2008.11.067 Blood 1

Data from ChEMBL 36 via Core Engine