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Compound Detail

CHEMBL95483

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CC(C)C[C@@H](C(=O)N1CCCCC1)[C@H](O)C(=O)NO

Basic Information

ChEMBL ID CHEMBL95483
Phase Preclinical
Structure Type MOL
InChI Key DYYRCQAVWNBEBP-MNOVXSKESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

272.4
MW (Da)
0.53
ALogP
4
HBA
3
HBD
89.9
PSA (Ų)
0.50
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H24N2O4
MW 272.35
Aromatic Rings 0
Heavy Atoms 19
NP-Likeness -0.21

Activity Summary

IC50 3 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.3 6.3 500.0 1
Interstitial collagenase
CHEMBL332
IC50 6.1 6.1 800.0 1
Neutrophil collagenase
CHEMBL4588
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 500.0 nM 6.3 Inhibition of Gel-A MMP-2 10522712
Interstitial collagenase IC50 = 800.0 nM 6.1 Inhibition of HFC MMP-1 10522712
Neutrophil collagenase IC50 = 1000.0 nM 6.0 Inhibition of HNC MMP-8 10522712

Literature References

PubMed DOI Target Context # Activities
10522712 10.1016/s0960-894x(99)00494-1 Interstitial collagenase 1
10522712 10.1016/s0960-894x(99)00494-1 72 kDa type IV collagenase 1
10522712 10.1016/s0960-894x(99)00494-1 Stromelysin-1 1
10522712 10.1016/s0960-894x(99)00494-1 Neutrophil collagenase 1
10522712 10.1016/s0960-894x(99)00494-1 Collagenase 3 1

Data from ChEMBL 36 via Core Engine