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Compound Detail

CHEMBL3233887

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CC(C)c1cccc(NC(=O)c2ccnc3cc(-c4ccc([C@H]5CC[C@H](CC(=O)O)CC5)cc4)ccc23)c1

Basic Information

ChEMBL ID CHEMBL3233887
Phase Preclinical
Structure Type MOL
InChI Key IKMARAMDTRCOCT-YHBQERECSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
8.03
ALogP
3
HBA
2
HBD
79.3
PSA (Ų)
0.27
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34N2O3
MW 506.65
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.71

Activity Summary

IC50 2 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Diacylglycerol O-acyltransferase 1
CHEMBL1075284
IC50 7.64 7.64 23.0 1
Diacylglycerol O-acyltransferase 1
CHEMBL6009
IC50 7.24 7.24 58.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 15.2 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Diacylglycerol O-acyltransferase 1 IC50 = 23.0 nM 7.64 Inhibition of mouse DGAT1 24618302
Diacylglycerol O-acyltransferase 1 IC50 = 58.0 nM 7.24 Inhibition of human DGAT1 24618302

Literature References

PubMed DOI Target Context # Activities
24618302 10.1016/j.bmcl.2014.02.028 Plasma 3
24618302 10.1016/j.bmcl.2014.02.028 Diacylglycerol O-acyltransferase 1 2
24618302 10.1016/j.bmcl.2014.02.028 Mus musculus 1
24618302 10.1016/j.bmcl.2014.02.028 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine