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Compound Detail

CHEMBL345597

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O=C(O)[C@@H](Cc1c[nH]c2ccccc12)NS(=O)(=O)c1ccc(-c2nnn(-c3ccccc3)n2)cc1

Basic Information

ChEMBL ID CHEMBL345597
Phase Preclinical
Structure Type MOL
InChI Key NLABJQQLMHAJIL-JOCHJYFZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
2.78
ALogP
7
HBA
3
HBD
142.9
PSA (Ų)
0.30
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N6O4S
MW 488.53
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 7.72 7.72 19.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 7.5 7.5 32.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9484512 10.1021/jm9707582 Matrix metalloproteinase-9 1
9484512 10.1021/jm9707582 72 kDa type IV collagenase 1
9484512 10.1021/jm9707582 Interstitial collagenase 1
9484512 10.1021/jm9707582 Stromelysin-1 1
9484512 10.1021/jm9707582 Matrilysin 1
9484512 10.1021/jm9707582 Angiotensin-converting enzyme 1
9484512 10.1021/jm9707582 Neprilysin 1
9484512 10.1021/jm9707582 Endothelin-converting enzyme 1 1

Data from ChEMBL 36 via Core Engine