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Compound Detail

CHEMBL92828

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COC(=O)CCNC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CCCc1ccc(Cl)cc1)CC(=O)NO

Basic Information

ChEMBL ID CHEMBL92828
Phase Preclinical
Structure Type MOL
InChI Key IURHJAMYHLDNBR-IRLDBZIGSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

524.1
MW (Da)
3.31
ALogP
6
HBA
4
HBD
133.8
PSA (Ų)
0.17
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H38ClN3O6
MW 524.06
Aromatic Rings 1
Heavy Atoms 36
NP-Likeness -0.06

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 9.02 9.02 1.0 1
Interstitial collagenase
CHEMBL332
Ki 6.87 6.87 135.0 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 = 0.96 nM 9.02 Inhibition of the stromelysin enzyme. -
Interstitial collagenase Ki = 135.0 nM 6.87 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