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Compound Detail

CHEMBL2058204

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CNC(=O)c1cc(C(=O)NC)cc(-c2ccc(O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)c(C)c2)c1

Basic Information

ChEMBL ID CHEMBL2058204
Phase Preclinical
Structure Type MOL
InChI Key CPNXCPWXQQMNFG-WCZGSDDISA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
10
Publications
0
Known Names

Molecular Properties

460.5
MW (Da)
-0.44
ALogP
8
HBA
6
HBD
157.6
PSA (Ų)
0.34
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N2O8
MW 460.48
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.60

Activity Summary

IC50 1 meas. best 7.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Escherichia coli
CHEMBL354
IC50 7.14 7.14 73.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Not specified
T1/2 2.0 hr -
T1/2 2.0 hr Not specified

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Escherichia coli IC50 = 73.0 nM 7.14 Antibacterial activity against Escherichia coli K-12 ATCC 25404 assessed as inhi... 22449031

Literature References

PubMed DOI Target Context # Activities
27689912 10.1021/acs.jmedchem.6b00948 ADMET 4
27689912 10.1021/acs.jmedchem.6b00948 Escherichia coli 4
22449031 10.1021/jm300165m Unchecked 3
22449031 10.1021/jm300165m Nucleic Acid 2
22449031 10.1021/jm300165m ADMET 1
22449031 10.1021/jm300165m Escherichia coli 1
- 10.1039/C3MD00346A Mus musculus 1
27689912 10.1021/acs.jmedchem.6b00948 Type 1 fimbrin D-mannose specific adhesin 1
27689912 10.1021/acs.jmedchem.6b00948 Unchecked 1
35777073 10.1021/acs.jmedchem.1c01039 Type 1 fimbrin D-mannose specific adhesin 1

Data from ChEMBL 36 via Core Engine