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Compound Detail

CHEMBL379382

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O=C1c2c(c(-c3c(F)cccc3F)c3cccnc3c2O)CN1Cc1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL379382
Phase Preclinical
Structure Type MOL
InChI Key UJQHSSFAJLJAPH-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

420.4
MW (Da)
5.18
ALogP
3
HBA
1
HBD
53.4
PSA (Ų)
0.50
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H15F3N2O2
MW 420.39
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.63

Activity Summary

IC50 2 meas. best 6.48
EC50 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 7.96 7.96 11.0 1
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 6.48 6.475 330.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16723225 10.1016/j.bmcl.2006.05.016 No relevant target 1
16723225 10.1016/j.bmcl.2006.05.016 MT4 1
16723225 10.1016/j.bmcl.2006.05.016 Human immunodeficiency virus 1 1
16723225 10.1016/j.bmcl.2006.05.016 Human immunodeficiency virus type 1 integrase 1
19450984 10.1016/j.bmc.2009.04.058 Human immunodeficiency virus type 1 integrase 1

Data from ChEMBL 36 via Core Engine