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Compound Detail

CHEMBL93791

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

Basic Information

ChEMBL ID CHEMBL93791
Phase Preclinical
Structure Type MOL
InChI Key FWRANZUQAGPBMV-FTJBHMTQSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

516.7
MW (Da)
3.74
ALogP
5
HBA
4
HBD
110.8
PSA (Ų)
0.15
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 C29H48N4O4
MW 516.73
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness -0.11

Activity Summary

Ki 3 meas. best 10.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 10.7 10.7 0.0 1
Stromelysin-1
CHEMBL283
Ki 8.23 8.23 5.9 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 = 0.02 nM 10.7 Inhibition of the gelatinase-A enzyme. -
Stromelysin-1 Ki = 5.87 nM 8.23 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