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Compound Detail

CHEMBL467460

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CC(C)OC(=O)N1CCC([C@@H](NS(=O)(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C(=O)O)CC1

Basic Information

ChEMBL ID CHEMBL467460
Phase Preclinical
Structure Type MOL
InChI Key SMAMMQUTTZLMCT-LJQANCHMSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

534.6
MW (Da)
4.42
ALogP
6
HBA
2
HBD
113.0
PSA (Ų)
0.54
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25F3N2O6S2
MW 534.58
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 8.41 6.88 3.9 2
Interstitial collagenase
CHEMBL332
IC50 5.2 5.2 6370.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 3.9 nM 8.41 Inhibition of MMP13 19422229
Collagenase 3 IC50 = 4475.0 nM 5.35 Inhibition of MMP13 in presence of 1% bovine serum albumin 19422229
Interstitial collagenase IC50 = 6370.0 nM 5.2 Inhibition of MMP1 19422229

Literature References

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

Data from ChEMBL 36 via Core Engine