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Compound Detail

CHEMBL4176832

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O=c1[nH]c2scc(-c3ccccc3)c2c(=O)n1O

Basic Information

ChEMBL ID CHEMBL4176832
Phase Preclinical
Structure Type MOL
InChI Key MRHQBMPZNODPQD-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

260.3
MW (Da)
1.66
ALogP
5
HBA
2
HBD
75.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H8N2O3S
MW 260.27
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -0.78

Activity Summary

IC50 2 meas. best 7.0
EC50 1 meas. best 4.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 7.0 7.0 100.0 1
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 5.89 5.89 1300.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29031062 10.1016/j.ejmech.2017.09.054 Gag-Pol polyprotein 1
29031062 10.1016/j.ejmech.2017.09.054 Human immunodeficiency virus type 1 reverse transcriptase 1
29031062 10.1016/j.ejmech.2017.09.054 Human immunodeficiency virus type 1 integrase 1
29031062 10.1016/j.ejmech.2017.09.054 Human immunodeficiency virus 1 1
29031062 10.1016/j.ejmech.2017.09.054 CEM-SS 1

Data from ChEMBL 36 via Core Engine