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Compound Detail

CHEMBL3617405

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COc1ccc(-c2ccc(S(=O)(=O)N(OC(C)C)[C@H](CCNC(=O)Cc3ccccc3)C(=O)NO)cc2)cc1

Basic Information

ChEMBL ID CHEMBL3617405
Phase Preclinical
Structure Type MOL
InChI Key WVPKYEATTXWJLC-AREMUKBSSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

555.6
MW (Da)
3.32
ALogP
7
HBA
3
HBD
134.3
PSA (Ų)
0.22
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33N3O7S
MW 555.65
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.71

Activity Summary

IC50 6 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 9.6 9.6 0.2 1
72 kDa type IV collagenase
CHEMBL333
IC50 9.43 9.43 0.4 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.54 8.54 2.9 1
Matrix metalloproteinase-14
CHEMBL3869
IC50 7.6 7.6 25.0 1
Stromelysin-1
CHEMBL283
IC50 7.44 7.44 36.0 1
Interstitial collagenase
CHEMBL332
IC50 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26263024 10.1021/acs.jmedchem.5b00367 72 kDa type IV collagenase 1
26263024 10.1021/acs.jmedchem.5b00367 Interstitial collagenase 1
26263024 10.1021/acs.jmedchem.5b00367 Stromelysin-1 1
26263024 10.1021/acs.jmedchem.5b00367 Matrix metalloproteinase-9 1
26263024 10.1021/acs.jmedchem.5b00367 Collagenase 3 1
26263024 10.1021/acs.jmedchem.5b00367 Matrix metalloproteinase-14 1

Data from ChEMBL 36 via Core Engine