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Compound Detail

CHEMBL466657

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CCOc1ccc(-c2ccc(S(=O)(=O)N[C@@H](C(=O)O)C3CCN(S(C)(=O)=O)CC3)s2)cc1

Basic Information

ChEMBL ID CHEMBL466657
Phase Preclinical
Structure Type MOL
InChI Key LBRZHKNWLBUBRK-LJQANCHMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.6
MW (Da)
2.22
ALogP
7
HBA
2
HBD
130.1
PSA (Ų)
0.54
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 C20H26N2O7S3
MW 502.64
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.44

Activity Summary

IC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 7.9 7.405 12.7 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 12.7 nM 7.9 Inhibition of MMP13 19422229
Collagenase 3 IC50 = 123.0 nM 6.91 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