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Compound Detail

CHEMBL1256967

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CC1(C)[C@H](NC(=O)/C(=N\OCc2cc(=O)c(O)cn2O)c2csc(N)n2)C(=O)N1OS(=O)(=O)O

Basic Information

ChEMBL ID CHEMBL1256967
Phase Preclinical
Structure Type MOL
InChI Key KLFSEZJCLYBFKQ-WXYNYTDUSA-N
3
Targets
11
Activities
1
Assay Types
7
PK Parameters
20
Publications
0
Known Names

Molecular Properties

518.5
MW (Da)
-1.41
ALogP
14
HBA
5
HBD
236.0
PSA (Ų)
0.09
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H18N6O10S2
MW 518.49
Aromatic Rings 2
Heavy Atoms 34

Activity Summary

IC50 11 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.32 5.3633 48.0 9
AmpC
CHEMBL1255151
IC50 6.3 6.3 500.0 1
Beta-lactamase
CHEMBL1255130
IC50 5.57 5.57 2700.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1714.0 ng.hr.mL-1 Rattus norvegicus
CL 7.94 mL.min-1.g-1 Homo sapiens
CL 11.48 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 3.0 uL.min-1.(10^6cells)-1 Homo sapiens
CL 9.8 mL.min-1.kg-1 Rattus norvegicus
Fu 0.0047 - Homo sapiens
T1/2 0.27 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00095K Pseudomonas aeruginosa 51
20308379 10.1128/aac.01525-09 Pseudomonas aeruginosa 46
29336873 10.1016/j.bmcl.2018.01.006 Escherichia coli 45
20308379 10.1128/aac.01525-09 Unchecked 44
20308379 10.1128/aac.01525-09 Enterobacter cloacae 15
20308379 10.1128/aac.01525-09 Escherichia coli 13
24694215 10.1021/jm500219c Escherichia coli 12
20308379 10.1128/aac.01525-09 Klebsiella pneumoniae 11
20308379 10.1128/aac.01525-09 Acinetobacter baumannii 9
20308379 10.1128/aac.01525-09 NON-PROTEIN TARGET 9
20308379 10.1128/aac.01525-09 Stenotrophomonas maltophilia 7
20308379 10.1128/aac.01525-09 Serratia marcescens 5
- 10.6019/CHEMBL3301361 ADMET 5
20308379 10.1128/aac.01525-09 Providencia rettgeri 4
20308379 10.1128/aac.01525-09 Klebsiella oxytoca 4
28287720 10.1021/acs.jmedchem.6b01261 Rattus norvegicus 4
28287720 10.1021/acs.jmedchem.6b01261 Klebsiella pneumoniae 4
20308379 10.1128/aac.01525-09 AmpC 4
20308379 10.1128/aac.01525-09 Beta-lactamase 4
20308379 10.1128/aac.01525-09 Providencia stuartii 3

Data from ChEMBL 36 via Core Engine