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Compound Detail

CHEMBL398641

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Cc1cc(C2CCN(S(=O)(=O)C(C)(C)C(=O)NO)CC2)ccc1-c1cccc(OCCO)c1

Basic Information

ChEMBL ID CHEMBL398641
Phase Preclinical
Structure Type MOL
InChI Key XMVZJCLXRBLZHB-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
2.83
ALogP
6
HBA
3
HBD
116.2
PSA (Ų)
0.40
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H32N2O6S
MW 476.60
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.47

Activity Summary

IC50 5 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
IC50 9.0 9.0 1.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 6.58 6.58 262.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 6.39 6.39 406.0 1
Matrix metalloproteinase-14
CHEMBL3869
IC50 5.77 5.77 1710.0 1
Interstitial collagenase
CHEMBL332
IC50 5.49 5.49 3230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 IC50 = 1.0 nM 9.0 Inhibition of MMP3 18029177
72 kDa type IV collagenase IC50 = 262.0 nM 6.58 Inhibition of MMP2 18029177
Matrix metalloproteinase-9 IC50 = 406.0 nM 6.39 Inhibition of MMP9 18029177
Matrix metalloproteinase-14 IC50 = 1710.0 nM 5.77 Inhibition of MMP14 18029177
Interstitial collagenase IC50 = 3230.0 nM 5.49 Inhibition of MMP1 18029177

Literature References

PubMed DOI Target Context # Activities
18029177 10.1016/j.bmcl.2007.10.042 Stromelysin-1 1
18029177 10.1016/j.bmcl.2007.10.042 72 kDa type IV collagenase 1
18029177 10.1016/j.bmcl.2007.10.042 Interstitial collagenase 1
18029177 10.1016/j.bmcl.2007.10.042 Matrix metalloproteinase-9 1
18029177 10.1016/j.bmcl.2007.10.042 Matrix metalloproteinase-14 1
18029177 10.1016/j.bmcl.2007.10.042 No relevant target 1

Data from ChEMBL 36 via Core Engine