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Compound Detail

CHEMBL456365

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CCOC(=O)/C(O)=C/C(=O)c1cn(Cc2ccc(F)cc2)c2cc(N3CCCC3)ccc2c1=O

Basic Information

ChEMBL ID CHEMBL456365
Phase Preclinical
Structure Type MOL
InChI Key ILTKHGJVTJFJEH-OYKKKHCWSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

464.5
MW (Da)
3.98
ALogP
7
HBA
1
HBD
88.8
PSA (Ų)
0.25
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25FN2O5
MW 464.49
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.92

Activity Summary

IC50 3 meas. best 5.64
EC50 2 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 6.08 5.735 830.0 2
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 5.64 5.605 2300.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18646746 10.1021/jm8001422 Human immunodeficiency virus type 1 integrase 4
24684270 10.1021/jm5001503 Human immunodeficiency virus type 1 reverse transcriptase 2
18646746 10.1021/jm8001422 Unchecked 1
18646746 10.1021/jm8001422 U-937 1
18646746 10.1021/jm8001422 Human immunodeficiency virus 1 1
24684270 10.1021/jm5001503 Human immunodeficiency virus 1 1
24684270 10.1021/jm5001503 HeLa 1
24684270 10.1021/jm5001503 Unchecked 1

Data from ChEMBL 36 via Core Engine