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Compound Detail

CHEMBL423686

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CC[C@@H](N[C@@H](CCc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)Nc1ccccc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL423686
Phase Preclinical
Structure Type MOL
InChI Key JUASDDPTEREPES-VJBWXMMDSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

453.6
MW (Da)
3.61
ALogP
4
HBA
4
HBD
107.5
PSA (Ų)
0.37
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H35N3O4
MW 453.58
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.24

Activity Summary

Ki 3 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
Ki 6.46 6.46 350.0 1
72 kDa type IV collagenase
CHEMBL333
Ki 5.96 5.96 1100.0 1
Interstitial collagenase
CHEMBL332
Ki 5.75 5.75 1800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 Ki = 350.0 nM 6.46 Inhibition of MMP-3. -
72 kDa type IV collagenase Ki = 1100.0 nM 5.96 Inhibition of MMP-2. -
Interstitial collagenase Ki = 1800.0 nM 5.75 Inhibition of matrix metalloprotease -1. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00024-8 Stromelysin-1 1
- 10.1016/0960-894X(96)00024-8 Interstitial collagenase 1
- 10.1016/0960-894X(96)00024-8 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine