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Compound Detail

CHEMBL306412

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

Basic Information

ChEMBL ID CHEMBL306412
Phase Preclinical
Structure Type MOL
InChI Key QRXOZHSEEGNRFC-PWSUYJOCSA-N

Known Names

Ro-37-9790
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
1
Known Names

Molecular Properties

315.4
MW (Da)
0.82
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 C15H29N3O4
MW 315.41
Aromatic Rings 0
Heavy Atoms 22
NP-Likeness 0.53

Activity Summary

IC50 3 meas. best 8.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase
CHEMBL2095216
IC50 8.31 8.31 4.9 1
Matrix metalloproteinase-9
CHEMBL321
IC50 7.98 7.98 10.4 1
Stromelysin-1
CHEMBL283
IC50 6.8 6.8 160.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 3.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase IC50 = 4.9 nM 8.31 Inhibition of human collagenase (MMP1) -
Matrix metalloproteinase-9 IC50 = 10.4 nM 7.98 Inhibition of human gelatinase B, MMP9 -
Stromelysin-1 IC50 = 160.0 nM 6.8 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