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Compound Detail

CHEMBL167302

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CCCc1ccc(CC[C@H](N[C@H](CCCCN2C(=O)c3ccccc3C2=O)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)Nc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL167302
Phase Preclinical
Structure Type MOL
InChI Key HCRZKUHDDTVHQM-GMTSZFNJSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

668.8
MW (Da)
5.62
ALogP
6
HBA
4
HBD
144.9
PSA (Ų)
0.10
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H48N4O6
MW 668.84
Aromatic Rings 3
Heavy Atoms 49
NP-Likeness -0.34

Activity Summary

Ki 2 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
Ki 8.72 8.72 1.9 1
72 kDa type IV collagenase
CHEMBL333
Ki 8.59 8.59 2.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 Ki = 1.9 nM 8.72 Inhibition of matrix metalloprotease-3 (MMP-3). -
72 kDa type IV collagenase Ki = 2.6 nM 8.59 Inhibition of matrix metalloprotease-2 (MMP-2) -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00109-6 Mus musculus 2
- 10.1016/0960-894X(96)00109-6 Stromelysin-1 1
- 10.1016/0960-894X(96)00109-6 Interstitial collagenase 1
- 10.1016/0960-894X(96)00109-6 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine