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Compound Detail

CHEMBL115263

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NC(=O)CNC(=O)[C@@H]1CCCCNC(=O)OCCC[C@H](C(=O)NO)[C@@H](Cc2ccc(-c3ccccc3C(F)(F)F)cc2)C(=O)N1

Basic Information

ChEMBL ID CHEMBL115263
Phase Preclinical
Structure Type MOL
InChI Key SOPDPCOBVSOXIM-ZDXQCDESSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

635.6
MW (Da)
2.43
ALogP
7
HBA
6
HBD
188.9
PSA (Ų)
0.20
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36F3N5O7
MW 635.64
Aromatic Rings 2
Heavy Atoms 45
NP-Likeness -0.24

Activity Summary

Ki 5 meas. best 8.82
IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3332
Ki 8.82 8.82 1.5 1
Homo sapiens
CHEMBL372
IC50 6.75 6.75 180.0 1
Neutrophil collagenase
CHEMBL4588
Ki 6.37 6.37 428.0 1
Collagenase 3
CHEMBL280
Ki 6.36 6.36 442.0 1
Matrilysin
CHEMBL4073
Ki 5.87 5.87 1336.0 1
72 kDa type IV collagenase
CHEMBL333
Ki 5.73 5.73 1867.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11585440 10.1021/jm0155502 Disintegrin and metalloproteinase domain-containing protein 17 1
11585440 10.1021/jm0155502 Homo sapiens 1
11585440 10.1021/jm0155502 Interstitial collagenase 1
11585440 10.1021/jm0155502 72 kDa type IV collagenase 1
11585440 10.1021/jm0155502 Matrix metalloproteinase-9 1
11585440 10.1021/jm0155502 Stromelysin-1 1
11585440 10.1021/jm0155502 Matrilysin 1
11585440 10.1021/jm0155502 Neutrophil collagenase 1
11585440 10.1021/jm0155502 Stromelysin-2 1
11585440 10.1021/jm0155502 Macrophage metalloelastase 1
11585440 10.1021/jm0155502 Collagenase 3 1
11585440 10.1021/jm0155502 Matrix metalloproteinase-14 1
11585440 10.1021/jm0155502 Matrix metalloproteinase-15 1
11585440 10.1021/jm0155502 Matrix metalloproteinase-16 1

Data from ChEMBL 36 via Core Engine