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Compound Detail

CHEMBL4096462

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NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)NO)Cc1cc(-c2ccc(-c3cccc(Cl)c3)cc2)no1

Basic Information

ChEMBL ID CHEMBL4096462
Phase Preclinical
Structure Type MOL
InChI Key VBMQORMYXJZHKU-OIBXWCBGSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

658.1
MW (Da)
1.90
ALogP
9
HBA
7
HBD
251.2
PSA (Ų)
0.08
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H32ClN5O10
MW 658.06
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.47

Activity Summary

Ki 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-2
CHEMBL4270
Ki 8.85 8.85 1.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-2 Ki = 1.4 nM 8.85 Inhibition of human MMP10 catalytic domain using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg... 27996256

Literature References

PubMed DOI Target Context # Activities
27996256 10.1021/acs.jmedchem.6b01420 Stromelysin-2 1
27996256 10.1021/acs.jmedchem.6b01420 Collagenase 3 1

Data from ChEMBL 36 via Core Engine