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Compound Detail

CHEMBL248172

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Cc1cc(COc2ccc(C(=O)NC3COCC34C(=O)NC(=O)NC4=O)cc2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL248172
Phase Preclinical
Structure Type MOL
InChI Key CNPXAHGTJQERBN-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

474.5
MW (Da)
1.60
ALogP
7
HBA
3
HBD
135.7
PSA (Ų)
0.48
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H22N4O6
MW 474.47
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.57

Activity Summary

IC50 2 meas. best 7.36
Ki 1 meas. best 5.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3332
IC50 7.36 7.36 44.0 1
Collagenase 3
CHEMBL280
Ki 5.45 5.45 3530.0 1
Blood
CHEMBL613416
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17027261 10.1016/j.bmcl.2006.09.048 Disintegrin and metalloproteinase domain-containing protein 17 1
17027261 10.1016/j.bmcl.2006.09.048 Stromelysin-1 1
17027261 10.1016/j.bmcl.2006.09.048 Matrilysin 1
17027261 10.1016/j.bmcl.2006.09.048 Macrophage metalloelastase 1
17027261 10.1016/j.bmcl.2006.09.048 Unchecked 1
17027261 10.1016/j.bmcl.2006.09.048 Blood 1
17027261 10.1016/j.bmcl.2006.09.048 72 kDa type IV collagenase 1
17027261 10.1016/j.bmcl.2006.09.048 Collagenase 3 1

Data from ChEMBL 36 via Core Engine