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Compound Detail

CHEMBL512275

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

Basic Information

ChEMBL ID CHEMBL512275
Phase Preclinical
Structure Type MOL
InChI Key IGDBRYFDPWPBAI-OAQYLSRUSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

510.6
MW (Da)
3.80
ALogP
7
HBA
2
HBD
122.2
PSA (Ų)
0.50
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30N2O7S2
MW 510.63
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.25

Activity Summary

IC50 3 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 9.0 8.045 1.0 2
Interstitial collagenase
CHEMBL332
IC50 5.03 5.03 9330.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 1.0 nM 9.0 Inhibition of MMP13 19422229
Collagenase 3 IC50 = 81.2 nM 7.09 Inhibition of MMP13 in presence of 1% bovine serum albumin 19422229
Interstitial collagenase IC50 = 9330.0 nM 5.03 Inhibition of MMP1 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