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Compound Detail

CHEMBL178509

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O=C1NC(=O)C2(CCC(=O)N2c2ccc(Oc3ccccc3)cc2)C(=O)N1

Basic Information

ChEMBL ID CHEMBL178509
Phase Preclinical
Structure Type MOL
InChI Key TVKGACNFKXXAEF-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
1.71
ALogP
5
HBA
2
HBD
104.8
PSA (Ų)
0.81
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H15N3O5
MW 365.35
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.32

Activity Summary

Ki 6 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 8.8 8.8 1.6 1
Collagenase 3
CHEMBL280
Ki 8.33 8.33 4.7 2
Matrix metalloproteinase-9
CHEMBL321
Ki 8.33 8.33 4.7 2
Stromelysin-1
CHEMBL283
Ki 5.35 5.35 4500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15686921 10.1016/j.bmcl.2004.12.016 Collagenase 3 1
15686921 10.1016/j.bmcl.2004.12.016 Interstitial collagenase 1
15686921 10.1016/j.bmcl.2004.12.016 72 kDa type IV collagenase 1
15686921 10.1016/j.bmcl.2004.12.016 Stromelysin-1 1
15686921 10.1016/j.bmcl.2004.12.016 Matrix metalloproteinase-9 1
15686921 10.1016/j.bmcl.2004.12.016 Disintegrin and metalloproteinase domain-containing protein 17 1
17275314 10.1016/j.bmc.2007.01.011 Matrix metalloproteinase-9 1
17275314 10.1016/j.bmc.2007.01.011 Collagenase 3 1

Data from ChEMBL 36 via Core Engine