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Compound Detail

CHEMBL4871381

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COc1ccc(NC(=O)[C@H]2Oc3c(c(=O)oc4ccccc34)[C@@H]2c2ccc(CCCN3CCCC3=O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4871381
Phase Preclinical
Structure Type MOL
InChI Key GHBDBTVKTLLIOR-FIBWVYCGSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

538.6
MW (Da)
4.89
ALogP
6
HBA
1
HBD
98.1
PSA (Ų)
0.32
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H30N2O6
MW 538.60
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.40

Activity Summary

Kd 1 meas. best 4.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MecA
CHEMBL6187
Kd 4.06 4.06 86600.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 2.46 10^4/M/s Staphylococcus aureus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MecA Kd = 86600.0 nM 4.06 Binding affinity to Staphylococcus aureus PBP2a assessed as equilibrium dissocia... 33811991

Literature References

PubMed DOI Target Context # Activities
33811991 10.1016/j.bmcl.2021.128001 MecA 3
33811991 10.1016/j.bmcl.2021.128001 Staphylococcus aureus 2
33811991 10.1016/j.bmcl.2021.128001 L02 1

Data from ChEMBL 36 via Core Engine