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Compound Detail

CHEMBL272871

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Cc1nn(C)c(C)c1S(=O)(=O)N(C)C1CCCn2c1nc(C(=O)NCc1ccc(F)cc1)c(O)c2=O

Basic Information

ChEMBL ID CHEMBL272871
Phase Preclinical
Structure Type MOL
InChI Key UMFNMQJGSPMGBC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

518.6
MW (Da)
1.52
ALogP
9
HBA
2
HBD
139.4
PSA (Ų)
0.50
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27FN6O5S
MW 518.57
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.15 8.15 7.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 7.0 nM 8.15 Inhibition of recombinant HIV1 integrase strand transfer activity 18217703

Literature References

PubMed DOI Target Context # Activities
18217703 10.1021/jm701164t Human immunodeficiency virus 1 2
18217703 10.1021/jm701164t Liver microsomes 2
18217703 10.1021/jm701164t Unchecked 1
18217703 10.1021/jm701164t Liver 1

Data from ChEMBL 36 via Core Engine