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Compound Detail

CHEMBL5562205

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Nc1ccc(-c2ccc(CC3CCNCC3)c(S(N)(=O)=O)c2-c2nn[nH]n2)cn1

Basic Information

ChEMBL ID CHEMBL5562205
Phase Preclinical
Structure Type MOL
InChI Key ASWFMIGVWSBZCA-UHFFFAOYSA-N
2
Targets
7
Activities
1
Assay Types
6
PK Parameters
6
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
0.70
ALogP
8
HBA
4
HBD
165.6
PSA (Ų)
0.47
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H22N8O2S
MW 414.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.47

Activity Summary

IC50 7 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.92 7.26 12.0 6
Metallo-beta-lactamase type 2
CHEMBL5465386
IC50 7.91 7.91 12.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 11.7 uM.hr Rattus norvegicus
CL 3.5 mL.min-1.kg-1 Rattus norvegicus
Cmax 16300.0 nM Rattus norvegicus
Cmax 791000.0 nM Rattus norvegicus
Fu 0.47 - Rattus norvegicus
MRT 1.21 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38387069 10.1021/acs.jmedchem.3c01614 ADMET 7
38387069 10.1021/acs.jmedchem.3c01614 Unchecked 4
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