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Compound Detail

CHEMBL401453

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Cc1cc(Cc2ccc(C(=O)N[C@@H]3CN(C(=O)C(C)(C)C)C[C@@H]3C(=O)NO)cc2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL401453
Phase Preclinical
Structure Type MOL
InChI Key JRRSWIJDZJXIAR-LADGPHEKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

488.6
MW (Da)
3.24
ALogP
5
HBA
3
HBD
111.6
PSA (Ų)
0.38
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 C28H32N4O4
MW 488.59
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.82

Activity Summary

IC50 2 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3332
IC50 8.82 8.82 1.5 1
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
IC50 7.02 7.02 95.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17276676 10.1016/j.bmcl.2007.01.041 Disintegrin and metalloproteinase domain-containing protein 17 2
17276676 10.1016/j.bmcl.2007.01.041 Caco-2 1
17276676 10.1016/j.bmcl.2007.01.041 Interstitial collagenase 1
17276676 10.1016/j.bmcl.2007.01.041 72 kDa type IV collagenase 1
17276676 10.1016/j.bmcl.2007.01.041 Matrix metalloproteinase-9 1
17276676 10.1016/j.bmcl.2007.01.041 Collagenase 3 1

Data from ChEMBL 36 via Core Engine