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Compound Detail

CHEMBL337946

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CSc1ccc(-c2ccc(S[C@H]3CC[C@@H](Cn4nnc5ccccc5c4=O)[C@@H]3C(=O)O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL337946
Phase Preclinical
Structure Type MOL
InChI Key DAAIDRXNEKWJIQ-LQGLAIQGSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

503.6
MW (Da)
5.45
ALogP
7
HBA
1
HBD
85.1
PSA (Ų)
0.34
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N3O3S2
MW 503.65
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.84

Activity Summary

IC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrix metalloproteinase-9
CHEMBL321
IC50 8.4 8.4 4.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 8.3 8.3 5.0 1
Collagenase 3
CHEMBL280
IC50 7.89 7.89 13.0 1
Stromelysin-1
CHEMBL283
IC50 7.68 7.68 21.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12930146 10.1021/jm0307638 Interstitial collagenase 1
12930146 10.1021/jm0307638 72 kDa type IV collagenase 1
12930146 10.1021/jm0307638 Stromelysin-1 1
12930146 10.1021/jm0307638 Matrix metalloproteinase-9 1
12930146 10.1021/jm0307638 Collagenase 3 1

Data from ChEMBL 36 via Core Engine