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Compound Detail

CHEMBL237384

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CC(C)[C@H](C(=O)NO)N(Cc1cccnc1)S(=O)(=O)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL237384
Phase Preclinical
Structure Type MOL
InChI Key PMSJHLLBCDOJAE-MRXNPFEDSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

381.4
MW (Da)
1.94
ALogP
5
HBA
2
HBD
99.6
PSA (Ų)
0.56
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 C17H20FN3O4S
MW 381.43
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.39

Activity Summary

IC50 4 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.92 6.92 120.0 1
Neutrophil collagenase
CHEMBL4588
IC50 6.64 6.64 228.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 6.38 6.38 414.0 1
Collagenase 3
CHEMBL280
IC50 6.28 6.28 527.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 120.0 nM 6.92 Inhibition of MMP2 17956082
Neutrophil collagenase IC50 = 228.0 nM 6.64 Inhibition of MMP8 17956082
Matrix metalloproteinase-9 IC50 = 414.0 nM 6.38 Inhibition of MMP9 17956082
Collagenase 3 IC50 = 527.0 nM 6.28 Inhibition of MMP13 17956082

Literature References

PubMed DOI Target Context # Activities
17956082 10.1021/jm0708533 72 kDa type IV collagenase 1
17956082 10.1021/jm0708533 Neutrophil collagenase 1
17956082 10.1021/jm0708533 Matrix metalloproteinase-9 1
17956082 10.1021/jm0708533 Collagenase 3 1

Data from ChEMBL 36 via Core Engine