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Compound Detail

CHEMBL392394

GS-39783
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CSc1nc(NC2CCCC2)c([N+](=O)[O-])c(NC2CCCC2)n1

Basic Information

ChEMBL ID CHEMBL392394
Name GS-39783
Phase Preclinical
Structure Type MOL
InChI Key GSGVDKOCBKBMGG-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

337.4
MW (Da)
3.82
ALogP
7
HBA
2
HBD
93.0
PSA (Ų)
0.35
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C15H23N5O2S
MW 337.45
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -1.16

Activity Summary

EC50 2 meas. best 7.1
IC50 1 meas. best 4.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid type B receptor subunit 1
CHEMBL2064
EC50 7.1 7.1 79.4 1
GABA-B receptor
CHEMBL2111463
EC50 6.13 6.13 741.3 1
NIH3T3
CHEMBL614822
IC50 4.22 4.22 60000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 U2OS 304
- 10.6019/CHEMBL5724801 Fibroblast 304
- 10.6019/CHEMBL5724801 HEK-293T 304
- 10.6019/CHEMBL5058577 Fibroblast 304
- 10.6019/CHEMBL5058577 U2OS 304
- 10.6019/CHEMBL5058577 HEK-293T 304
23544432 10.1021/jm400144w Mus musculus 21
- 10.6019/CHEMBL5058564 Fibroblast 6
- 10.6019/CHEMBL5058564 U2OS 6
- 10.6019/CHEMBL5058564 HEK-293T 5
17884493 10.1016/j.bmcl.2007.09.023 GABA-B receptor 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
28408223 10.1016/j.bmcl.2017.03.084 Gamma-aminobutyric acid type B receptor subunit 1 3
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
- 10.6019/CHEMBL5209801 G-protein coupled receptor 35 2
- 10.6019/CHEMBL5209801 Type-1 angiotensin II receptor 2
- 10.6019/CHEMBL5209801 Sphingosine 1-phosphate receptor 1 2
- 10.6019/CHEMBL5209801 C5a anaphylatoxin chemotactic receptor 1 2
- 10.6019/CHEMBL5209801 Alpha-2A adrenergic receptor 2

Data from ChEMBL 36 via Core Engine