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Compound Detail

CHEMBL468095

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CCOC(=O)N1CCC([C@@H](NS(=O)(=O)c2ccc(-c3ccc(OCC)cc3)s2)C(=O)O)CC1

Basic Information

ChEMBL ID CHEMBL468095
Phase Preclinical
Structure Type MOL
InChI Key VOHDRNMYQAWLKL-HXUWFJFHSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

496.6
MW (Da)
3.41
ALogP
7
HBA
2
HBD
122.2
PSA (Ų)
0.55
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O7S2
MW 496.61
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.31

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 8.7 7.775 2.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 2.0 nM 8.7 Inhibition of MMP13 19422229
Collagenase 3 IC50 = 142.0 nM 6.85 Inhibition of MMP13 in presence of 1% bovine serum albumin 19422229

Literature References

PubMed DOI Target Context # Activities
19422229 10.1021/jm801394m Collagenase 3 2
19422229 10.1021/jm801394m Interstitial collagenase 1
19422229 10.1021/jm801394m Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine