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Compound Detail

CHEMBL236565

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CC(C)[C@H](C(=O)O)N(Cc1ccccc1)S(=O)(=O)c1ccc(OCCI)cc1

Basic Information

ChEMBL ID CHEMBL236565
Phase Preclinical
Structure Type MOL
InChI Key REIYGWGAFRRHED-LJQANCHMSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

517.4
MW (Da)
3.80
ALogP
4
HBA
1
HBD
83.9
PSA (Ų)
0.38
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24INO5S
MW 517.39
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.74

Activity Summary

IC50 2 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.68 6.68 207.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 5.87 5.87 1350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 207.0 nM 6.68 Inhibition of MMP2 17956082
Matrix metalloproteinase-9 IC50 = 1350.0 nM 5.87 Inhibition of MMP9 17956082

Literature References

PubMed DOI Target Context # Activities
17956082 10.1021/jm0708533 72 kDa type IV collagenase 1
17956082 10.1021/jm0708533 Neutrophil collagenase 1
17956082 10.1021/jm0708533 Matrix metalloproteinase-9 1
17956082 10.1021/jm0708533 Collagenase 3 1

Data from ChEMBL 36 via Core Engine