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Compound Detail

CHEMBL1223541

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CN(C)S(=O)(=O)N1C[C@@H](F)C[C@H]1c1nc(C(=O)NCc2ccc(F)cc2)c(O)c(=O)n1C

Basic Information

ChEMBL ID CHEMBL1223541
Phase Preclinical
Structure Type MOL
InChI Key UOFGXMDVJQLSIB-KBPBESRZSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.5
MW (Da)
0.45
ALogP
7
HBA
2
HBD
124.8
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H23F2N5O5S
MW 471.49
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 8.05 8.05 9.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Rattus norvegicus
CL 64.0 mL.min-1.kg-1 Rattus norvegicus
F 16.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 integrase IC50 = 9.0 nM 8.05 Inhibition of HIV 1 recombinant integrase 20674351

Literature References

PubMed DOI Target Context # Activities
20674351 10.1016/j.bmcl.2010.07.042 Rattus norvegicus 4
20674351 10.1016/j.bmcl.2010.07.042 Human immunodeficiency virus 1 2
20674351 10.1016/j.bmcl.2010.07.042 Human immunodeficiency virus type 1 integrase 1

Data from ChEMBL 36 via Core Engine