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Compound Detail

CHEMBL439944

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CNC(=O)[C@H](NC(=O)[C@H](CC(C)C)[C@@H](C)C(=O)NO)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL439944
Phase Preclinical
Structure Type MOL
InChI Key WWNOVCQMRIZSRV-UTUOFQBUSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

329.4
MW (Da)
1.07
ALogP
4
HBA
4
HBD
107.5
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H31N3O4
MW 329.44
Aromatic Rings 0
Heavy Atoms 23
NP-Likeness 0.52

Activity Summary

IC50 3 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 8.62 8.62 2.4 1
Collagenase
CHEMBL2095216
IC50 8.59 8.59 2.6 1
Stromelysin-1
CHEMBL283
IC50 7.33 7.33 47.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 2.7 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrix metalloproteinase-9 IC50 = 2.4 nM 8.62 Inhibition of human gelatinase B, MMP9 -
Collagenase IC50 = 2.6 nM 8.59 Inhibition of human collagenase (MMP1) -
Stromelysin-1 IC50 = 47.0 nM 7.33 Inhibition of human stromelysin-1, MMP-3 -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00416-2 Collagenase 1
- 10.1016/S0960-894X(97)00416-2 Stromelysin-1 1
- 10.1016/S0960-894X(97)00416-2 Matrix metalloproteinase-9 1
- 10.1016/S0960-894X(97)00416-2 No relevant target 1
- 10.1016/S0960-894X(97)00416-2 ADMET 1

Data from ChEMBL 36 via Core Engine