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Compound Detail

CHEMBL3238124

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CCOC(=O)/C(O)=C/C(=O)c1cn(Cc2ccc(F)cc2)c2cc(N3CCOCC3)ccc2c1=O

Basic Information

ChEMBL ID CHEMBL3238124
Phase Preclinical
Structure Type MOL
InChI Key XADUGWSFXAXZBS-OYKKKHCWSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

480.5
MW (Da)
3.21
ALogP
8
HBA
1
HBD
98.1
PSA (Ų)
0.24
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 C26H25FN2O6
MW 480.49
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.03

Activity Summary

EC50 1 meas. best 4.79
IC50 1 meas. best 5.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 5.68 5.68 2100.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 4.79 4.79 16200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24684270 10.1021/jm5001503 Human immunodeficiency virus type 1 integrase 2
24684270 10.1021/jm5001503 Human immunodeficiency virus type 1 reverse transcriptase 2
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