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Compound Detail

CHEMBL204100

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

Basic Information

ChEMBL ID CHEMBL204100
Phase Preclinical
Structure Type MOL
InChI Key XNLVNQQMTWGGIM-HOCLYGCPSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

427.6
MW (Da)
0.81
ALogP
7
HBA
3
HBD
122.0
PSA (Ų)
0.35
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H25N3O5S2
MW 427.55
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.60

Activity Summary

IC50 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interstitial collagenase
CHEMBL332
IC50 7.68 7.68 21.0 1
Collagenase 3
CHEMBL280
IC50 7.62 7.62 24.0 1
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
IC50 7.24 7.24 57.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Interstitial collagenase IC50 = 21.0 nM 7.68 Inhibition of MMP1 16426848
Collagenase 3 IC50 = 24.0 nM 7.62 Inhibition of MMP13 16426848
Disintegrin and metalloproteinase domain-containing protein 17 IC50 = 57.0 nM 7.24 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