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Compound Detail

CHEMBL26058

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CC(=O)N1CCC([C@H](C(=O)NO)[C@@H](Cc2cccc(O)c2)C(=O)N[C@H]2c3ccccc3C[C@H]2O)CC1

Basic Information

ChEMBL ID CHEMBL26058
Phase Preclinical
Structure Type MOL
InChI Key JCFYPSQTTQQSEU-NGSHPTGOSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

495.6
MW (Da)
1.71
ALogP
6
HBA
5
HBD
139.2
PSA (Ų)
0.29
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N3O6
MW 495.58
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness 0.20

Activity Summary

IC50 1 meas. best 7.54
Ki 1 meas. best 5.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.54 7.54 29.0 1
Matrix metalloproteinase-9
CHEMBL321
Ki 5.76 5.76 1741.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 29.0 nM 7.54 Inhibition of bovine aggrecanase 12657268
Matrix metalloproteinase-9 Ki = 1741.0 nM 5.76 Affinity for Matrix metalloprotease-9 (MMP-9) 12657268

Literature References

PubMed DOI Target Context # Activities
12657268 10.1016/s0960-894x(03)00124-0 Unchecked 1
12657268 10.1016/s0960-894x(03)00124-0 Matrix metalloproteinase-9 1

Data from ChEMBL 36 via Core Engine