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Compound Detail

CHEMBL236974

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

Basic Information

ChEMBL ID CHEMBL236974
Phase Preclinical
Structure Type MOL
InChI Key YJBLORWBSQLNFW-MRXNPFEDSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

408.4
MW (Da)
1.71
ALogP
7
HBA
2
HBD
142.7
PSA (Ų)
0.38
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 C17H20N4O6S
MW 408.44
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.38

Activity Summary

IC50 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 8.0 8.0 10.0 1
Neutrophil collagenase
CHEMBL4588
IC50 7.85 7.85 14.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 6.12 6.12 756.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 5.29 5.29 5150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 10.0 nM 8.0 Inhibition of MMP13 17956082
Neutrophil collagenase IC50 = 14.0 nM 7.85 Inhibition of MMP8 17956082
72 kDa type IV collagenase IC50 = 756.0 nM 6.12 Inhibition of MMP2 17956082
Matrix metalloproteinase-9 IC50 = 5150.0 nM 5.29 Inhibition of MMP9 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