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Compound Detail

CHEMBL250266

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COC[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCc1ccc(-c2ccccc2)c(C)c1)CC(=O)O)C(C)(C)C)c1ccccc1

Basic Information

ChEMBL ID CHEMBL250266
Phase Preclinical
Structure Type MOL
InChI Key NSMABJUGSNPHMN-BHYWQNONSA-N
5
Targets
10
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

572.8
MW (Da)
6.11
ALogP
4
HBA
3
HBD
104.7
PSA (Ų)
0.22
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H44N2O5
MW 572.75
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness 0.24

Activity Summary

IC50 10 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
IC50 7.64 7.64 23.0 2
Collagenase 3
CHEMBL280
IC50 5.64 5.64 2300.0 2
Matrix metalloproteinase-9
CHEMBL321
IC50 4.52 4.52 30400.0 2
72 kDa type IV collagenase
CHEMBL333
IC50 4.47 4.47 34200.0 2
Matrix metalloproteinase-14
CHEMBL3869
IC50 4.17 4.17 66900.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18029177 10.1016/j.bmcl.2007.10.042 Stromelysin-1 1
18029177 10.1016/j.bmcl.2007.10.042 72 kDa type IV collagenase 1
18029177 10.1016/j.bmcl.2007.10.042 Interstitial collagenase 1
18029177 10.1016/j.bmcl.2007.10.042 Matrix metalloproteinase-9 1
18029177 10.1016/j.bmcl.2007.10.042 Collagenase 3 1
18029177 10.1016/j.bmcl.2007.10.042 Matrix metalloproteinase-14 1
18790648 10.1016/j.bmc.2008.08.058 Interstitial collagenase 1
18790648 10.1016/j.bmc.2008.08.058 Matrix metalloproteinase-14 1
18790648 10.1016/j.bmc.2008.08.058 Matrix metalloproteinase-9 1
18790648 10.1016/j.bmc.2008.08.058 Collagenase 3 1
18790648 10.1016/j.bmc.2008.08.058 Stromelysin-1 1
18790648 10.1016/j.bmc.2008.08.058 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine