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Compound Detail

CHEMBL401404

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COc1cccc(N[C@@H](CN(c2ccc(Oc3ccc(C)cc3)cc2)S(C)(=O)=O)C(=O)NO)c1

Basic Information

ChEMBL ID CHEMBL401404
Phase Preclinical
Structure Type MOL
InChI Key MXIFPAKFUUYAMN-QHCPKHFHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
3.55
ALogP
7
HBA
3
HBD
117.2
PSA (Ų)
0.30
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27N3O6S
MW 485.56
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 9.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 9.21 9.21 0.6 1
72 kDa type IV collagenase
CHEMBL333
IC50 7.57 7.57 27.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrix metalloproteinase-9 IC50 = 0.62 nM 9.21 Inhibition of MMP9 18083558
72 kDa type IV collagenase IC50 = 27.0 nM 7.57 Inhibition of MMP2 18083558

Literature References

PubMed DOI Target Context # Activities
18083558 10.1016/j.bmcl.2007.11.129 72 kDa type IV collagenase 1
18083558 10.1016/j.bmcl.2007.11.129 Matrix metalloproteinase-9 1
18083558 10.1016/j.bmcl.2007.11.129 Unchecked 1
18083558 10.1016/j.bmcl.2007.11.129 Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine