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Compound Detail

CHEMBL202932

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COc1ccc(-c2ccc(S(=O)(=O)N[C@@H](C(C)C)P(=O)(O)O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL202932
Phase Preclinical
Structure Type MOL
InChI Key BZVYQWLRCHLAGK-QGZVFWFLSA-N
9
Targets
12
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
2.80
ALogP
4
HBA
3
HBD
112.9
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C17H22NO6PS
MW 399.41
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.58

Activity Summary

IC50 8 meas. best 8.85
Ki 4 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil collagenase
CHEMBL4588
Ki 9.22 9.22 0.6 1
Unchecked
CHEMBL612545
Ki 9.22 9.22 0.6 1
Neutrophil collagenase
CHEMBL4588
IC50 8.85 8.85 1.4 1
72 kDa type IV collagenase
CHEMBL333
IC50 8.82 8.82 1.5 1
Collagenase 3
CHEMBL280
IC50 8.59 8.59 2.6 1
72 kDa type IV collagenase
CHEMBL333
Ki 8.3 8.3 5.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.1 8.1 8.0 1
Stromelysin-1
CHEMBL283
Ki 7.4 7.4 40.0 1
Stromelysin-1
CHEMBL283
IC50 7.28 7.28 52.0 1
Matrix metalloproteinase-14
CHEMBL3869
IC50 7.1 7.1 79.0 1
Interstitial collagenase
CHEMBL332
IC50 6.82 6.82 150.0 1
Matrilysin
CHEMBL4073
IC50 6.34 6.34 460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16451058 10.1021/jm050787+ 72 kDa type IV collagenase 1
16451058 10.1021/jm050787+ Stromelysin-1 1
16451058 10.1021/jm050787+ Neutrophil collagenase 1
17088065 10.1016/j.bmc.2006.10.047 Interstitial collagenase 1
17088065 10.1016/j.bmc.2006.10.047 72 kDa type IV collagenase 1
17088065 10.1016/j.bmc.2006.10.047 Stromelysin-1 1
17088065 10.1016/j.bmc.2006.10.047 Matrilysin 1
17088065 10.1016/j.bmc.2006.10.047 Neutrophil collagenase 1
17088065 10.1016/j.bmc.2006.10.047 Matrix metalloproteinase-9 1
17088065 10.1016/j.bmc.2006.10.047 Collagenase 3 1
17088065 10.1016/j.bmc.2006.10.047 Matrix metalloproteinase-14 1
17228863 10.1021/jm0608457 Unchecked 1

Data from ChEMBL 36 via Core Engine