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Compound Detail

CHEMBL41892

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CC(=O)N(O)CCOc1ccc(-c2ccc(C#N)cc2)cc1

Basic Information

ChEMBL ID CHEMBL41892
Phase Preclinical
Structure Type MOL
InChI Key ZOQRCAUTYNYRRI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

296.3
MW (Da)
2.84
ALogP
4
HBA
1
HBD
73.6
PSA (Ų)
0.68
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H16N2O3
MW 296.33
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.68

Activity Summary

IC50 2 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stromelysin-1
CHEMBL283
IC50 5.4 5.4 4000.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 5.23 5.23 5900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stromelysin-1 IC50 = 4000.0 nM 5.4 In vitro inhibition of Matrix metalloprotease-3 11412979
72 kDa type IV collagenase IC50 = 5900.0 nM 5.23 In vitro inhibition of Matrix metalloprotease-2 11412979

Literature References

PubMed DOI Target Context # Activities
11412979 10.1016/s0960-894x(01)00031-2 72 kDa type IV collagenase 1
11412979 10.1016/s0960-894x(01)00031-2 Stromelysin-1 1
11412979 10.1016/s0960-894x(01)00031-2 Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine