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Compound Detail

CHEMBL3238132

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

Basic Information

ChEMBL ID CHEMBL3238132
Phase Preclinical
Structure Type MOL
InChI Key MKDDADZFUNGYKM-UUYOSTAYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
2.73
ALogP
7
HBA
2
HBD
109.1
PSA (Ų)
0.34
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 C24H21FN2O6
MW 452.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.94

Activity Summary

IC50 3 meas. best 7.1
EC50 1 meas. best 4.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 7.1 5.995 80.0 2
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 5.17 5.17 6800.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 4.58 4.58 26300.0 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 3
24684270 10.1021/jm5001503 Human immunodeficiency virus type 1 reverse transcriptase 3
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