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Compound Detail

CHEMBL222002

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CCOCCC1(Oc2ccc(Oc3ccc(F)cc3)cc2)C(=O)NC(=O)NC1=O

Basic Information

ChEMBL ID CHEMBL222002
Phase Preclinical
Structure Type MOL
InChI Key XRSYNYGEEYTXJV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
2.53
ALogP
6
HBA
2
HBD
103.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19FN2O6
MW 402.38
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.38

Activity Summary

IC50 2 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 9.22 9.22 0.6 1
Matrix metalloproteinase-14
CHEMBL3869
IC50 7.64 7.64 22.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 0.6 nM 9.22 Inhibition of MMP13 17935984
Matrix metalloproteinase-14 IC50 = 22.91 nM 7.64 Inhibition of MMP14 17275314

Literature References

PubMed DOI Target Context # Activities
17935984 10.1016/j.bmcl.2007.09.085 Unchecked 2
17935984 10.1016/j.bmcl.2007.09.085 Collagenase 3 1
17935984 10.1016/j.bmcl.2007.09.085 MMP-2/MMP-13 1
17275314 10.1016/j.bmc.2007.01.011 Matrix metalloproteinase-14 1

Data from ChEMBL 36 via Core Engine