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Compound Detail

CHEMBL254509

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CNC(=O)C1CCN([C@@H](CN(c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2)S(C)(=O)=O)C(=O)NO)CC1

Basic Information

ChEMBL ID CHEMBL254509
Phase Preclinical
Structure Type MOL
InChI Key NXDUTDHMFGWNPY-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

558.6
MW (Da)
2.60
ALogP
7
HBA
3
HBD
128.3
PSA (Ų)
0.32
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29F3N4O6S
MW 558.58
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.33

Activity Summary

IC50 2 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 8.6 8.6 2.5 1
72 kDa type IV collagenase
CHEMBL333
IC50 8.26 8.26 5.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrix metalloproteinase-9 IC50 = 2.5 nM 8.6 Inhibition of MMP9 18083558
72 kDa type IV collagenase IC50 = 5.5 nM 8.26 Inhibition of MMP2 18083558

Literature References

PubMed DOI Target Context # Activities
18083558 10.1016/j.bmcl.2007.11.129 72 kDa type IV collagenase 1
18083558 10.1016/j.bmcl.2007.11.129 Matrix metalloproteinase-9 1
18083558 10.1016/j.bmcl.2007.11.129 Unchecked 1

Data from ChEMBL 36 via Core Engine