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Compound Detail

CHEMBL8973

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CC(C)Cc1cccc(-c2ccccc2C(C)C)c1O[C@@H]1C[C@@H](CNC(=O)c2ccc(/C=C3\SC(=O)NC3=O)cc2)N(C(=O)c2ccccc2C(=O)c2ccc(F)cc2)C1

Basic Information

ChEMBL ID CHEMBL8973
Phase Preclinical
Structure Type MOL
InChI Key QJBZDMABLBVIPO-UERFOIPISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

824.0
MW (Da)
9.46
ALogP
7
HBA
2
HBD
121.9
PSA (Ų)
0.09
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C49H46FN3O6S
MW 823.99
Aromatic Rings 5
Heavy Atoms 60
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytosolic phospholipase A2
CHEMBL3816
IC50 8.28 8.28 5.3 1
THP-1
CHEMBL614245
IC50 7.04 7.04 92.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10737736 10.1021/jm9905155 Cytosolic phospholipase A2 1
10737736 10.1021/jm9905155 THP-1 1

Data from ChEMBL 36 via Core Engine