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Compound Detail

CHEMBL82487

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COc1ccc(S(=O)(=O)N(Cc2cccnc2)c2c(C(=O)NO)csc2Br)cc1

Basic Information

ChEMBL ID CHEMBL82487
Phase Preclinical
Structure Type MOL
InChI Key OCVZODLPTGAJKD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

498.4
MW (Da)
3.43
ALogP
7
HBA
2
HBD
108.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16BrN3O5S2
MW 498.38
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.51

Activity Summary

IC50 2 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 7.16 7.16 70.0 1
Collagenase 3
CHEMBL280
IC50 6.54 6.54 290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrix metalloproteinase-9 IC50 = 70.0 nM 7.16 Inhibition of Matrix metalloprotease-9 11206468
Collagenase 3 IC50 = 290.0 nM 6.54 Inhibition of Matrix metalloprotease-13 11206468

Literature References

PubMed DOI Target Context # Activities
11206468 10.1016/s0960-894x(00)00644-2 Interstitial collagenase 1
11206468 10.1016/s0960-894x(00)00644-2 Matrix metalloproteinase-9 1
11206468 10.1016/s0960-894x(00)00644-2 Collagenase 3 1
11206468 10.1016/s0960-894x(00)00644-2 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine