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Compound Detail

CHEMBL79712

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Cc1cc(C)cc(CC[C@H](N[C@H](C)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)Nc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL79712
Phase Preclinical
Structure Type MOL
InChI Key NNDUTDPDZHXRRE-QDSKXPNFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
3.84
ALogP
4
HBA
4
HBD
107.5
PSA (Ų)
0.38
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H37N3O4
MW 467.61
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.23

Activity Summary

Ki 1 meas. best 5.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 5.32 5.32 4840.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 4840.0 nM 5.32 Inhibitory activity against human gelatinase-A (MMP-2) -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00425-S Stromelysin-1 1
- 10.1016/0960-894X(95)00425-S Interstitial collagenase 1
- 10.1016/0960-894X(95)00425-S 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine