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Compound Detail

CHEMBL112508

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CC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)N[C@H](CCCCCNC(=O)Cc1ccccc1)C(=O)O)C(=O)Nc1ccccc1

Basic Information

ChEMBL ID CHEMBL112508
Phase Preclinical
Structure Type MOL
InChI Key OLFNQERWBAAFKD-DSPMFFIESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

628.8
MW (Da)
5.12
ALogP
5
HBA
5
HBD
136.6
PSA (Ų)
0.11
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H48N4O5
MW 628.81
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.29

Activity Summary

Ki 3 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
Ki 7.33 7.33 47.0 1
72 kDa type IV collagenase
CHEMBL333
Ki 6.46 6.46 350.0 1
Interstitial collagenase
CHEMBL332
Ki 5.24 5.24 5810.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 Ki = 47.0 nM 7.33 Inhibition of MMP-3. -
72 kDa type IV collagenase Ki = 350.0 nM 6.46 Inhibition of MMP-2. -
Interstitial collagenase Ki = 5810.0 nM 5.24 Inhibition of matrix metalloprotease -1. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00024-8 Stromelysin-1 1
- 10.1016/0960-894X(96)00024-8 Interstitial collagenase 1
- 10.1016/0960-894X(96)00024-8 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine