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Compound Detail

CHEMBL468096

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

Basic Information

ChEMBL ID CHEMBL468096
Phase Preclinical
Structure Type MOL
InChI Key KLPSRFNMJRNHAH-JOCHJYFZSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

524.7
MW (Da)
4.19
ALogP
7
HBA
2
HBD
122.2
PSA (Ų)
0.42
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H32N2O7S2
MW 524.66
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.17

Activity Summary

IC50 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 9.1 8.075 0.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 0.8 nM 9.1 Inhibition of MMP13 19422229
Collagenase 3 IC50 = 90.0 nM 7.05 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