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Compound Detail

CHEMBL4278928

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O=c1cc(Sc2ccc(-c3ccc(F)cc3)cc2)[nH]c(=O)n1O

Basic Information

ChEMBL ID CHEMBL4278928
Phase Preclinical
Structure Type MOL
InChI Key ZGVHBCQIOBUKGW-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

330.3
MW (Da)
2.73
ALogP
5
HBA
2
HBD
75.1
PSA (Ų)
0.57
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11FN2O3S
MW 330.34
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.72

Activity Summary

EC50 1 meas. best 4.92
IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 8.22 8.22 6.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30031976 10.1016/j.ejmech.2018.07.039 Unchecked 2
30031976 10.1016/j.ejmech.2018.07.039 Human immunodeficiency virus type 1 reverse transcriptase 1
30031976 10.1016/j.ejmech.2018.07.039 Gag-Pol polyprotein 1
30031976 10.1016/j.ejmech.2018.07.039 Human immunodeficiency virus type 1 integrase 1
30031976 10.1016/j.ejmech.2018.07.039 Human immunodeficiency virus 1 1
34147908 10.1016/j.ejmech.2021.113640 Tripartite terminase subunit 3 1
34147908 10.1016/j.ejmech.2021.113640 Unchecked 1
34147908 10.1016/j.ejmech.2021.113640 HEL 299 1

Data from ChEMBL 36 via Core Engine