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Compound Detail

CHEMBL252823

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CC(C)N(CCNC(=O)OCc1ccccc1)[C@@H](CN(c1ccc(Oc2ccc(C(F)(F)F)cc2)cc1)S(C)(=O)=O)C(=O)NO

Basic Information

ChEMBL ID CHEMBL252823
Phase Preclinical
Structure Type MOL
InChI Key YQDBAVJLVOFOMZ-MHZLTWQESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

652.7
MW (Da)
4.77
ALogP
8
HBA
3
HBD
137.5
PSA (Ų)
0.17
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35F3N4O7S
MW 652.69
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 7.54 7.54 29.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 6.58 6.58 262.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrix metalloproteinase-9 IC50 = 29.0 nM 7.54 Inhibition of MMP9 18083558
72 kDa type IV collagenase IC50 = 262.0 nM 6.58 Inhibition of MMP2 18083558

Literature References

PubMed DOI Target Context # Activities
18083558 10.1016/j.bmcl.2007.11.129 72 kDa type IV collagenase 1
18083558 10.1016/j.bmcl.2007.11.129 Matrix metalloproteinase-9 1
18083558 10.1016/j.bmcl.2007.11.129 Unchecked 1

Data from ChEMBL 36 via Core Engine