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Compound Detail

CHEMBL247967

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Cc1cc(COc2ccc(C(=O)NC3CCCC34C(=O)NC(=O)NC4=O)cc2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL247967
Phase Preclinical
Structure Type MOL
InChI Key YYHXOYNNTNFXCS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

472.5
MW (Da)
2.76
ALogP
6
HBA
3
HBD
126.5
PSA (Ų)
0.49
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 C26H24N4O5
MW 472.50
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.41

Activity Summary

IC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3332
IC50 7.62 7.62 24.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Disintegrin and metalloproteinase domain-containing protein 17 IC50 = 24.0 nM 7.62 Inhibition of porcine TACE 17027261

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