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Compound Detail

CHEMBL91054

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CC(C)Cc1ccc(CCC[C@H](CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)NCCc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL91054
Phase Preclinical
Structure Type MOL
InChI Key NEPPMULRSZAPIH-JSOSNVBQSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

548.8
MW (Da)
6.11
ALogP
3
HBA
3
HBD
95.5
PSA (Ų)
0.24
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H48N2O4
MW 548.77
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness 0.13

Activity Summary

Ki 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 6.8 6.8 157.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 157.0 nM 6.8 Inhibition of the Gelatinase-A enzyme was determined from purified NSO cells. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80588-6 72 kDa type IV collagenase 1
- 10.1016/S0960-894X(01)80588-6 Stromelysin-1 1
- 10.1016/S0960-894X(01)80588-6 Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine