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Compound Detail

CHEMBL4847813

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Cc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCN(C(=O)CNC(=O)OC(C)(C)C)CC2)cc1

Basic Information

ChEMBL ID CHEMBL4847813
Phase Preclinical
Structure Type MOL
InChI Key UMWMGHMFFNFXNI-SANMLTNESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
3.91
ALogP
5
HBA
4
HBD
132.6
PSA (Ų)
0.33
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C31H39N5O5
MW 561.68
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -1.24

Activity Summary

Kd 1 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MecA
CHEMBL6187
Kd 6.89 6.89 129.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 3.28 10^5/M/s Staphylococcus aureus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MecA Kd = 129.0 nM 6.89 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 Staphylococcus aureus 28
33811991 10.1016/j.bmcl.2021.128001 MecA 3
- 10.6019/CHEMBL4888484 Plasmodium falciparum 2
33811991 10.1016/j.bmcl.2021.128001 L02 1

Data from ChEMBL 36 via Core Engine