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Compound Detail

CHEMBL590113

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COc1cccc2c(S(=O)(=O)NC(=O)Nc3ncc(Br)s3)cn(C)c12

Basic Information

ChEMBL ID CHEMBL590113
Phase Preclinical
Structure Type MOL
InChI Key UYENKFIAVMJNOD-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

445.3
MW (Da)
2.92
ALogP
7
HBA
2
HBD
102.3
PSA (Ų)
0.64
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H13BrN4O4S2
MW 445.32
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.54

Activity Summary

EC50 1 meas. best 4.85
IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fructose-1,6-bisphosphatase 1
CHEMBL3975
IC50 7.16 7.16 70.0 1
Fructose-1,6-bisphosphatase 1
CHEMBL5360
EC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fructose-1,6-bisphosphatase 1 IC50 = 70.0 nM 7.16 Inhibition of FBPase in human liver 19969452
Fructose-1,6-bisphosphatase 1 EC50 = 14000.0 nM 4.85 Inhibition of FBPase in mouse liver 19969452

Literature References

PubMed DOI Target Context # Activities
19969452 10.1016/j.bmcl.2009.11.093 Fructose-1,6-bisphosphatase 1 2

Data from ChEMBL 36 via Core Engine