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Compound Detail

CHEMBL205998

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CC#CCOc1ccc(S(=O)(=O)N2C[C@H](CCN(CC)CC)SC(C)(C)[C@@H]2C(=O)NO)cc1

Basic Information

ChEMBL ID CHEMBL205998
Phase Preclinical
Structure Type MOL
InChI Key BUSXTPHZLBAFDD-FPOVZHCZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

497.7
MW (Da)
2.58
ALogP
7
HBA
2
HBD
99.2
PSA (Ų)
0.29
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H35N3O5S2
MW 497.68
Aromatic Rings 1
Heavy Atoms 33
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interstitial collagenase
CHEMBL332
IC50 7.48 7.48 33.0 1
Collagenase 3
CHEMBL280
IC50 7.32 7.32 48.0 1
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
IC50 6.84 6.84 143.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Interstitial collagenase IC50 = 33.0 nM 7.48 Inhibition of MMP1 16426848
Collagenase 3 IC50 = 48.0 nM 7.32 Inhibition of MMP13 16426848
Disintegrin and metalloproteinase domain-containing protein 17 IC50 = 143.0 nM 6.84 Inhibition of TACE 16426848

Literature References

PubMed DOI Target Context # Activities
16426848 10.1016/j.bmcl.2005.12.020 Disintegrin and metalloproteinase domain-containing protein 17 3
16426848 10.1016/j.bmcl.2005.12.020 Interstitial collagenase 1
16426848 10.1016/j.bmcl.2005.12.020 Collagenase 3 1
16426848 10.1016/j.bmcl.2005.12.020 Mus musculus 1

Data from ChEMBL 36 via Core Engine