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Compound Detail

CHEMBL1766816

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COCCN(C)c1ncc(NC(=O)c2nc(-c3ccccc3)oc2C(F)(F)F)cn1

Basic Information

ChEMBL ID CHEMBL1766816
Phase Preclinical
Structure Type MOL
InChI Key ZQOHEEKXXKJSHZ-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

421.4
MW (Da)
3.49
ALogP
7
HBA
1
HBD
93.4
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18F3N5O3
MW 421.38
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.70

Activity Summary

EC50 1 meas. best 6.27
IC50 1 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Diacylglycerol O-acyltransferase 1
CHEMBL6009
IC50 7.32 7.32 48.0 1
Diacylglycerol O-acyltransferase 1
CHEMBL6009
EC50 6.27 6.27 534.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21413799 10.1021/jm101580m Diacylglycerol O-acyltransferase 1 2
21413799 10.1021/jm101580m Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine