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Compound Detail

CHEMBL92453

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Cc1ccc(CCC[C@H](CC(=O)NO)C(=O)N[C@@H](CC2CCCCC2)C(=O)NCCc2ccc(S(N)(=O)=O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL92453
Phase Preclinical
Structure Type MOL
InChI Key WYEWOIOFHXNSNW-IAPPQJPRSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

600.8
MW (Da)
3.29
ALogP
6
HBA
5
HBD
167.7
PSA (Ų)
0.16
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H44N4O6S
MW 600.78
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness -0.28

Activity Summary

Ki 3 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 11.0 11.0 0.0 1
Stromelysin-1
CHEMBL283
Ki 8.53 8.53 3.0 1
Interstitial collagenase
CHEMBL332
Ki 6.48 6.48 329.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 0.01 nM 11.0 Inhibition of the gelatinase-A enzyme. -
Stromelysin-1 Ki = 2.98 nM 8.53 Inhibition of the stromelysin enzyme. -
Interstitial collagenase Ki = 329.0 nM 6.48 Inhibition of the collagenase enzyme. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80587-4 72 kDa type IV collagenase 1
- 10.1016/S0960-894X(01)80587-4 Stromelysin-1 1
- 10.1016/S0960-894X(01)80587-4 Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine