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Compound Detail

CHEMBL267939

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COc1ccc(S(=O)(=O)N2CCN(C(=O)OCc3ccccc3)CC[C@@H]2C(=O)NO)cc1

Basic Information

ChEMBL ID CHEMBL267939
Phase Preclinical
Structure Type MOL
InChI Key XDYZXHJJAIXYOR-LJQANCHMSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

463.5
MW (Da)
1.60
ALogP
7
HBA
2
HBD
125.5
PSA (Ų)
0.49
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N3O7S
MW 463.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.31

Activity Summary

IC50 7 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 8.8 8.8 1.6 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.74 8.74 1.8 1
Collagenase 3
CHEMBL4944
IC50 8.68 8.68 2.1 1
Neutrophil collagenase
CHEMBL4588
IC50 8.48 8.48 3.3 1
Stromelysin-1
CHEMBL283
IC50 7.85 7.85 14.0 1
Interstitial collagenase
CHEMBL332
IC50 7.01 7.01 97.0 1
Matrilysin
CHEMBL4073
IC50 6.13 6.13 737.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11327577 10.1016/s0960-894x(01)00137-8 Interstitial collagenase 1
11327577 10.1016/s0960-894x(01)00137-8 72 kDa type IV collagenase 1
11327577 10.1016/s0960-894x(01)00137-8 Stromelysin-1 1
11327577 10.1016/s0960-894x(01)00137-8 Matrilysin 1
11327577 10.1016/s0960-894x(01)00137-8 Neutrophil collagenase 1
11327577 10.1016/s0960-894x(01)00137-8 Matrix metalloproteinase-9 1
11327577 10.1016/s0960-894x(01)00137-8 Collagenase 3 1

Data from ChEMBL 36 via Core Engine