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Compound Detail

CHEMBL1766806

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COC(=O)N1CCC(c2ccc(NC(=O)c3nc(-c4ccccc4)oc3C(F)(F)F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL1766806
Phase Preclinical
Structure Type MOL
InChI Key RCXDLPPBDGCXNX-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

473.4
MW (Da)
5.56
ALogP
5
HBA
1
HBD
84.7
PSA (Ų)
0.54
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22F3N3O4
MW 473.45
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.37

Activity Summary

EC50 1 meas. best 6.43
IC50 1 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Diacylglycerol O-acyltransferase 1
CHEMBL6009
IC50 7.08 7.08 84.0 1
Diacylglycerol O-acyltransferase 1
CHEMBL6009
EC50 6.43 6.43 371.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 21.12 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21413799 10.1021/jm101580m Diacylglycerol O-acyltransferase 1 4
21413799 10.1021/jm101580m Voltage-gated inwardly rectifying potassium channel KCNH2 1
21413799 10.1021/jm101580m Mus musculus 1

Data from ChEMBL 36 via Core Engine