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Compound Detail

CHEMBL131051

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CSc1nc(-c2ccc(OC(F)(F)F)cc2)nn1C(=O)N(C)c1ccccc1

Basic Information

ChEMBL ID CHEMBL131051
Phase Preclinical
Structure Type MOL
InChI Key RKKAABIABTWSCU-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

408.4
MW (Da)
4.67
ALogP
6
HBA
0
HBD
60.2
PSA (Ų)
0.59
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 C18H15F3N4O2S
MW 408.40
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.80

Activity Summary

IC50 3 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hormone-sensitive lipase
CHEMBL5582
IC50 8.36 8.36 4.4 1
Hormone-sensitive lipase
CHEMBL3590
IC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14711311 10.1021/jm031004s Hormone-sensitive lipase 1
14711311 10.1021/jm031004s Acetylcholinesterase 1
14711311 10.1021/jm031004s Cholinesterase 1
14711311 10.1021/jm031004s Pancreatic triacylglycerol lipase 1
14711311 10.1021/jm031004s Lipoprotein lipase 1
14711311 10.1021/jm031004s Hepatic triacylglycerol lipase 1
18808096 10.1021/jm800718k Hormone-sensitive lipase 1
26222445 10.1021/acs.jmedchem.5b00434 Acetylcholinesterase 1
26222445 10.1021/acs.jmedchem.5b00434 Hormone-sensitive lipase 1

Data from ChEMBL 36 via Core Engine