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Compound Detail

CHEMBL253261

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COCCOC(=O)N1CCC(C(C(=O)O)N(Cc2cccnc2)S(=O)(=O)c2ccc(-c3ccc(OC)cc3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL253261
Phase Preclinical
Structure Type MOL
InChI Key APXZBXMVEOBZDS-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

597.7
MW (Da)
3.90
ALogP
8
HBA
1
HBD
135.6
PSA (Ų)
0.31
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35N3O8S
MW 597.69
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 8.52 8.52 3.0 1
Neutrophil collagenase
CHEMBL4588
IC50 8.49 8.49 3.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 3.02 nM 8.52 Inhibition of MMP13 17275314
Neutrophil collagenase IC50 = 3.236 nM 8.49 Inhibition of MMP8 17275314

Literature References

PubMed DOI Target Context # Activities
17275314 10.1016/j.bmc.2007.01.011 Collagenase 3 1
17275314 10.1016/j.bmc.2007.01.011 Neutrophil collagenase 1

Data from ChEMBL 36 via Core Engine