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Compound Detail

CHEMBL3337898

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COc1cccc(CNC(=O)c2nc3scc(CNC(=O)c4ccccc4)c3c(=O)[nH]2)c1

Basic Information

ChEMBL ID CHEMBL3337898
Phase Preclinical
Structure Type MOL
InChI Key UDNFOSNJEJROIQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

448.5
MW (Da)
2.85
ALogP
6
HBA
3
HBD
113.2
PSA (Ų)
0.40
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20N4O4S
MW 448.50
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.38

Activity Summary

IC50 1 meas. best 10.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 10.74 10.74 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2289.0 ng.hr.mL-1 Rattus norvegicus
CL 3.567 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 0.018 nM 10.74 Inhibition of human recombinant MMP13 catalytic domain using fluorescence peptid... 25192810

Literature References

PubMed DOI Target Context # Activities
25192810 10.1016/j.bmc.2014.07.025 Rattus norvegicus 3
25192810 10.1016/j.bmc.2014.07.025 Collagenase 3 1

Data from ChEMBL 36 via Core Engine