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Compound Detail

CHEMBL403778

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Cc1nc2ccccn2c1Cc1ccc(C(=O)N[C@@H]2CCOC[C@@H]2C(=O)NO)cc1

Basic Information

ChEMBL ID CHEMBL403778
Phase Preclinical
Structure Type MOL
InChI Key YXKKEOGFLPKGED-ZWKOTPCHSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
1.87
ALogP
6
HBA
3
HBD
105.0
PSA (Ų)
0.44
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 C22H24N4O4
MW 408.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 9.0
Ki 1 meas. best 5.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3332
IC50 9.0 9.0 1.0 1
Blood
CHEMBL613416
IC50 6.91 6.91 122.0 1
Macrophage metalloelastase
CHEMBL4393
Ki 5.99 5.99 1021.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18282708 10.1016/j.bmcl.2008.01.120 Unchecked 4
18282708 10.1016/j.bmcl.2008.01.120 Disintegrin and metalloproteinase domain-containing protein 17 1
18282708 10.1016/j.bmcl.2008.01.120 Blood 1
18282708 10.1016/j.bmcl.2008.01.120 72 kDa type IV collagenase 1
18282708 10.1016/j.bmcl.2008.01.120 Stromelysin-1 1
18282708 10.1016/j.bmcl.2008.01.120 Matrilysin 1
18282708 10.1016/j.bmcl.2008.01.120 Macrophage metalloelastase 1

Data from ChEMBL 36 via Core Engine