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Compound Detail

CHEMBL392088

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

Basic Information

ChEMBL ID CHEMBL392088
Phase Preclinical
Structure Type MOL
InChI Key BXSPGECKGKAUCR-GOSISDBHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

406.5
MW (Da)
1.87
ALogP
6
HBA
2
HBD
102.8
PSA (Ų)
0.51
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 C19H26N4O4S
MW 406.51
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.23

Activity Summary

IC50 4 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.0 6.0 992.0 1
Neutrophil collagenase
CHEMBL4588
IC50 5.92 5.92 1200.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 5.88 5.88 1330.0 1
Collagenase 3
CHEMBL280
IC50 5.87 5.87 1340.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 992.0 nM 6.0 Inhibition of MMP2 17956082
Neutrophil collagenase IC50 = 1200.0 nM 5.92 Inhibition of MMP8 17956082
Matrix metalloproteinase-9 IC50 = 1330.0 nM 5.88 Inhibition of MMP9 17956082
Collagenase 3 IC50 = 1340.0 nM 5.87 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