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Compound Detail

CHEMBL2375602

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COc1ccc(CNC(=O)[C@]2(C)[C@@H](OC(C)=O)CC[C@]3(C)[C@H]4[C@@H](O)c5c(cc(-c6cccnc6)oc5=O)O[C@]4(C)[C@@H](OC(=O)c4ccc(C#N)cc4)C[C@H]32)c(OC)c1

Basic Information

ChEMBL ID CHEMBL2375602
Phase Preclinical
Structure Type MOL
InChI Key YBPLVXSCROVJTQ-HIAYPNGJSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

791.9
MW (Da)
5.69
ALogP
13
HBA
2
HBD
196.5
PSA (Ų)
0.20
QED
3
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H45N3O11
MW 791.85
Aromatic Rings 4
Heavy Atoms 58
NP-Likeness 0.80

Activity Summary

IC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 2
CHEMBL4465
IC50 6.85 6.85 140.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 9.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 2 IC50 = 140.0 nM 6.85 Inhibition of ACAT2 (unknown origin) 23535327

Literature References

PubMed DOI Target Context # Activities
23535327 10.1016/j.bmcl.2013.02.088 Unchecked 1
23535327 10.1016/j.bmcl.2013.02.088 Sterol O-acyltransferase 1 1
23535327 10.1016/j.bmcl.2013.02.088 Sterol O-acyltransferase 2 1

Data from ChEMBL 36 via Core Engine