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Compound Detail

CHEMBL295950

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CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(=O)c1ccc[nH]1)CC(C)C

Basic Information

ChEMBL ID CHEMBL295950
Phase Preclinical
Structure Type MOL
InChI Key WGYOZKBKTQRASH-IERDGZPVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

422.5
MW (Da)
3.20
ALogP
3
HBA
4
HBD
106.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N4O3
MW 422.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.13

Activity Summary

IC50 2 meas. best 6.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.27 6.27 540.0 1
Interstitial collagenase
CHEMBL332
IC50 6.07 6.07 860.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 540.0 nM 6.27 Inhibition of Matrix metalloprotease-2 12729664
Interstitial collagenase IC50 = 860.0 nM 6.07 Inhibition of matrix metalloprotease-1 12729664

Literature References

PubMed DOI Target Context # Activities
12729664 10.1016/s0960-894x(03)00214-2 Interstitial collagenase 1
12729664 10.1016/s0960-894x(03)00214-2 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine