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Compound Detail

CHEMBL456325

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O=C(Nc1ccc2c(c1)C(=O)N(O)C(=O)C2)c1cccc([N+](=O)[O-])c1

Basic Information

ChEMBL ID CHEMBL456325
Phase Preclinical
Structure Type MOL
InChI Key SJRRAXJYEVBLAZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

341.3
MW (Da)
1.76
ALogP
6
HBA
2
HBD
129.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11N3O6
MW 341.28
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.22

Activity Summary

IC50 2 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 5.05 5.05 8900.0 1
Unchecked
CHEMBL612545
IC50 4.97 4.97 10800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 integrase IC50 = 8900.0 nM 5.05 Inhibition of HIV1 integrase 19053754
Unchecked IC50 = 10800.0 nM 4.97 Inhibition of HIV1 RNase H 19053754

Literature References

PubMed DOI Target Context # Activities
19053754 10.1021/jm8007085 Unchecked 2
19053754 10.1021/jm8007085 Human immunodeficiency virus type 1 integrase 1
19053754 10.1021/jm8007085 Human immunodeficiency virus 1 1
19053754 10.1021/jm8007085 MT4 1
19053754 10.1021/jm8007085 Human immunodeficiency virus type 1 reverse transcriptase 1

Data from ChEMBL 36 via Core Engine