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Compound Detail

CHEMBL452588

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O=S1(=O)CCCCN1c1nc(-c2nnc(Cc3ccc(F)cc3)[nH]2)c(O)c2ncccc12

Basic Information

ChEMBL ID CHEMBL452588
Phase Preclinical
Structure Type MOL
InChI Key CAWTUZMSASDZAZ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

454.5
MW (Da)
2.78
ALogP
7
HBA
2
HBD
125.0
PSA (Ų)
0.49
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19FN6O3S
MW 454.49
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.38

Activity Summary

EC50 1 meas. best 6.62
IC50 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 7.96 7.96 11.0 1
Human immunodeficiency virus
CHEMBL613758
EC50 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19217781 10.1016/j.bmcl.2009.01.090 Human immunodeficiency virus type 1 integrase 1
19217781 10.1016/j.bmcl.2009.01.090 Human immunodeficiency virus 1

Data from ChEMBL 36 via Core Engine