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Compound Detail

CHEMBL80102

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COc1cccc(CC[C@H](N[C@H](C)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)Nc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL80102
Phase Preclinical
Structure Type MOL
InChI Key UVCYZCWBCCZIRY-LEOXJPRUSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

469.6
MW (Da)
3.23
ALogP
5
HBA
4
HBD
116.8
PSA (Ų)
0.36
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H35N3O5
MW 469.58
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.28

Activity Summary

Ki 2 meas. best 5.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
Ki 5.33 5.33 4677.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 Ki = 4700.0 nM 5.33 Inhibitory activity against human stromelysin-3 (MMP-3) -
Stromelysin-1 Ki = 4677.35 nM 5.33 Inhibition of MMP3 17275314

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00425-S Stromelysin-1 1
- 10.1016/0960-894X(95)00425-S Interstitial collagenase 1
- 10.1016/0960-894X(95)00425-S 72 kDa type IV collagenase 1
17275314 10.1016/j.bmc.2007.01.011 Stromelysin-1 1

Data from ChEMBL 36 via Core Engine