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Compound Detail

CHEMBL4646018

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O=[N+]([O-])c1cccc(-c2nc3ccc(Br)cc3[nH]2)c1

Basic Information

ChEMBL ID CHEMBL4646018
Phase Preclinical
Structure Type MOL
InChI Key QRYNOBDMCSLODZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

318.1
MW (Da)
3.90
ALogP
3
HBA
1
HBD
71.8
PSA (Ų)
0.58
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H8BrN3O2
MW 318.13
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -1.57

Activity Summary

IC50 1 meas. best 4.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 4.33 4.33 47000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 47000.0 nM 4.33 Inhibition of recombinant human MMP13 catalytic domain (Tyr104 to Asn274 residue... 31874775

Literature References

PubMed DOI Target Context # Activities
31874775 10.1016/j.bmc.2019.115257 72 kDa type IV collagenase 1
31874775 10.1016/j.bmc.2019.115257 Neutrophil collagenase 1
31874775 10.1016/j.bmc.2019.115257 Matrix metalloproteinase-9 1
31874775 10.1016/j.bmc.2019.115257 Collagenase 3 1

Data from ChEMBL 36 via Core Engine