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Compound Detail

CHEMBL440921

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CSc1ccc(-c2ccc(S(=O)(=O)N[C@@H](C(=O)O)C(C)C)cc2)cc1

Basic Information

ChEMBL ID CHEMBL440921
Phase Preclinical
Structure Type MOL
InChI Key JDHBSANRAFEDMI-QGZVFWFLSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

379.5
MW (Da)
3.46
ALogP
4
HBA
2
HBD
83.5
PSA (Ų)
0.72
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 C18H21NO4S2
MW 379.50
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 7.64 7.64 23.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 7.4 7.4 40.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 189200.0 nM Mus musculus

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
9484512 10.1021/jm9707582 Mus musculus 1

Data from ChEMBL 36 via Core Engine