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Compound Detail

CHEMBL93695

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O=C(C[C@@H](CCCc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCCCCN1CCOCC1)NO

Basic Information

ChEMBL ID CHEMBL93695
Phase Preclinical
Structure Type MOL
InChI Key MWWSEQIBKWJTDA-VPUSJEBWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

579.2
MW (Da)
3.86
ALogP
6
HBA
4
HBD
120.0
PSA (Ų)
0.13
QED
1
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H47ClN4O5
MW 579.18
Aromatic Rings 1
Heavy Atoms 40
NP-Likeness -0.46

Activity Summary

Ki 3 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 10.52 10.52 0.0 1
Stromelysin-1
CHEMBL283
Ki 8.62 8.62 2.4 1
Interstitial collagenase
CHEMBL332
Ki 6.5 6.5 313.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 0.03 nM 10.52 Inhibition of the gelatinase-A enzyme. -
Stromelysin-1 Ki = 2.39 nM 8.62 Inhibition of the stromelysin enzyme. -
Interstitial collagenase Ki = 313.0 nM 6.5 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