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Compound Detail

CHEMBL2205735

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COC(=O)c1ccc2[nH]c(COc3ccc(C45CC6CC(CC(C6)C4)C5)cc3)nc2c1

Basic Information

ChEMBL ID CHEMBL2205735
Phase Preclinical
Structure Type MOL
InChI Key DDSDQTSUZNQOAY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
5.40
ALogP
4
HBA
1
HBD
64.2
PSA (Ų)
0.57
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28N2O3
MW 416.52
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 4.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Diacylglycerol O-acyltransferase 1
CHEMBL6129
IC50 4.64 4.64 23000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Diacylglycerol O-acyltransferase 1 IC50 = 23000.0 nM 4.64 Inhibition of DGAT in rat liver microsomes 23141914

Literature References

PubMed DOI Target Context # Activities
22305612 10.1016/j.ejmech.2012.01.033 MDA-MB-435 1
23141914 10.1016/j.bmcl.2012.10.046 Diacylglycerol O-acyltransferase 1 1

Data from ChEMBL 36 via Core Engine