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Compound Detail

CHEMBL36191

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COc1ccc(S(=O)(=O)N(Cc2ccccc2)c2c(C(=O)NO)cnc3ccc(Br)cc23)cc1

Basic Information

ChEMBL ID CHEMBL36191
Phase Preclinical
Structure Type MOL
InChI Key JAVKQWAQQAGPFN-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

542.4
MW (Da)
4.52
ALogP
6
HBA
2
HBD
108.8
PSA (Ų)
0.26
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20BrN3O5S
MW 542.41
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.24

Activity Summary

IC50 4 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 8.22 8.22 6.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.1 8.1 8.0 1
Interstitial collagenase
CHEMBL332
IC50 6.97 6.97 107.2 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12668018 10.1016/s0960-894x(03)00127-6 Interstitial collagenase 1
12668018 10.1016/s0960-894x(03)00127-6 Matrix metalloproteinase-9 1
12668018 10.1016/s0960-894x(03)00127-6 Collagenase 3 1
12668018 10.1016/s0960-894x(03)00127-6 Disintegrin and metalloproteinase domain-containing protein 17 1
17275314 10.1016/j.bmc.2007.01.011 Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine