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Compound Detail

CHEMBL2311891

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COc1cc(/C=N/Nc2ccc(S(=O)(=O)Nc3ccccc3C(=O)O)cc2[N+](=O)[O-])ccc1O

Basic Information

ChEMBL ID CHEMBL2311891
Phase Preclinical
Structure Type MOL
InChI Key LZJWACDYXIPMKB-WSDLNYQXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

486.5
MW (Da)
3.25
ALogP
9
HBA
4
HBD
180.5
PSA (Ų)
0.20
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N4O8S
MW 486.46
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.39

Activity Summary

IC50 1 meas. best 4.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 25000.0 nM 4.6 Inhibition of human Flag-tagged LEDGF interaction to His6-tagged HIV1 integrase ... 23306052

Literature References

PubMed DOI Target Context # Activities
23306052 10.1016/j.bmc.2012.12.012 Human immunodeficiency virus type 1 integrase 2
23306052 10.1016/j.bmc.2012.12.012 Human immunodeficiency virus 1 1
23306052 10.1016/j.bmc.2012.12.012 Unchecked 1

Data from ChEMBL 36 via Core Engine