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Compound Detail

CHEMBL5565123

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NS(=O)(=O)c1c(C(F)(F)F)ccc([C@H]2CC[C@H](N)CC2)c1-c1nn[nH]n1

Basic Information

ChEMBL ID CHEMBL5565123
Phase Preclinical
Structure Type MOL
InChI Key QLFUPIPMVYHNSD-ZKCHVHJHSA-N
2
Targets
6
Activities
1
Assay Types
10
PK Parameters
6
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
1.52
ALogP
6
HBA
3
HBD
140.6
PSA (Ų)
0.73
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H17F3N6O2S
MW 390.39
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.00

Activity Summary

IC50 6 meas. best 9.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.18 8.204 0.7 5
Metallo-beta-lactamase type 2
CHEMBL5465386
IC50 7.87 7.87 13.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5.0 uM.hr Rattus norvegicus
AUC 16.7 uM.hr Canis lupus familiaris
CL 8.7 mL.min-1.kg-1 Rattus norvegicus
CL 2.6 mL.min-1.kg-1 Canis lupus familiaris
Cmax 12700.0 nM Rattus norvegicus
Cmax 15000.0 nM Canis lupus familiaris
Fu 0.78 - Rattus norvegicus
Fu 0.76 - Canis lupus familiaris
MRT 0.87 hr Rattus norvegicus
MRT 2.03 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38387069 10.1021/acs.jmedchem.3c01614 ADMET 13
38387069 10.1021/acs.jmedchem.3c01614 Unchecked 3
38387069 10.1021/acs.jmedchem.3c01614 Pseudomonas aeruginosa 3
38387069 10.1021/acs.jmedchem.3c01614 Escherichia coli 1
38387069 10.1021/acs.jmedchem.3c01614 Serratia marcescens 1
38387069 10.1021/acs.jmedchem.3c01614 Klebsiella pneumoniae 1

Data from ChEMBL 36 via Core Engine