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Compound Detail

CHEMBL77808

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O=C(C[C@@H](CCc1ccccc1)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCCc1ccccc1)NO

Basic Information

ChEMBL ID CHEMBL77808
Phase Preclinical
Structure Type MOL
InChI Key FCKWIYZMPDIGLV-FTJBHMTQSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
3.95
ALogP
4
HBA
4
HBD
107.5
PSA (Ų)
0.25
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39N3O4
MW 493.65
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness 0.11

Activity Summary

Ki 6 meas. best 8.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 8.65 8.65 2.2 2
Stromelysin-1
CHEMBL283
Ki 7.11 7.11 77.0 2
Interstitial collagenase
CHEMBL332
Ki 6.21 6.21 618.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11428927 10.1021/jm001090l Interstitial collagenase 1
11428927 10.1021/jm001090l 72 kDa type IV collagenase 1
11428927 10.1021/jm001090l Stromelysin-1 1
- 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