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Compound Detail

CHEMBL520785

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O=S(=O)(CCC(S)CS)c1ccc(Oc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL520785
Phase Preclinical
Structure Type MOL
InChI Key VALKNOMNTXYCBM-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

354.5
MW (Da)
3.87
ALogP
5
HBA
2
HBD
43.4
PSA (Ų)
0.74
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 C16H18O3S3
MW 354.52
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.84

Activity Summary

Ki 4 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 7.34 7.34 46.0 1
Matrix metalloproteinase-9
CHEMBL321
Ki 7.0 7.0 100.0 1
Matrix metalloproteinase-14
CHEMBL3869
Ki 6.68 6.68 210.0 1
Stromelysin-1
CHEMBL283
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 46.0 nM 7.34 Inhibition of MMP2 18790648
Matrix metalloproteinase-9 Ki = 100.0 nM 7.0 Inhibition of MMP9 18790648
Matrix metalloproteinase-14 Ki = 210.0 nM 6.68 Inhibition of MMP14 18790648
Stromelysin-1 Ki = 10000.0 nM 5.0 Inhibition of MMP3 18790648

Literature References

PubMed DOI Target Context # Activities
18790648 10.1016/j.bmc.2008.08.058 Matrilysin 1
18790648 10.1016/j.bmc.2008.08.058 Interstitial collagenase 1
18790648 10.1016/j.bmc.2008.08.058 Matrix metalloproteinase-14 1
18790648 10.1016/j.bmc.2008.08.058 Matrix metalloproteinase-9 1
18790648 10.1016/j.bmc.2008.08.058 Stromelysin-1 1
18790648 10.1016/j.bmc.2008.08.058 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine