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Compound Detail

CHEMBL10296

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O=C(Nc1ccc(S(=O)(=O)NC(CC#CCN2CCOCC2)C(=O)O)cc1)c1ccc(Br)cc1

Basic Information

ChEMBL ID CHEMBL10296
Phase Preclinical
Structure Type MOL
InChI Key AWDSUFIHUSMPAR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

550.4
MW (Da)
2.16
ALogP
6
HBA
3
HBD
125.0
PSA (Ų)
0.43
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24BrN3O6S
MW 550.43
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.40

Activity Summary

IC50 3 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 7.92 7.92 12.0 1
Collagenase 3
CHEMBL280
IC50 6.46 6.46 344.0 1
Stromelysin-1
CHEMBL283
IC50 4.76 4.76 17400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11297453 10.1021/jm000477l Interstitial collagenase 1
11297453 10.1021/jm000477l 72 kDa type IV collagenase 1
11297453 10.1021/jm000477l Stromelysin-1 1
11297453 10.1021/jm000477l Collagenase 3 1
11297453 10.1021/jm000477l No relevant target 1

Data from ChEMBL 36 via Core Engine