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Compound Detail

CHEMBL2398806

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Cc1cccc([C@@H]2OC[C@@]3(C)[C@@H]4C[C@H](OC(=O)c5ccc(C#N)cc5)[C@@]5(C)Oc6cc(-c7cccnc7)oc(=O)c6[C@H](O)[C@@H]5[C@@]4(C)CC[C@@H]3O2)c1

Basic Information

ChEMBL ID CHEMBL2398806
Phase Preclinical
Structure Type MOL
InChI Key WSBKXEFDERVRCY-KFSBURAESA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

688.8
MW (Da)
6.85
ALogP
10
HBA
1
HBD
141.1
PSA (Ų)
0.23
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H40N2O8
MW 688.78
Aromatic Rings 4
Heavy Atoms 51
NP-Likeness 1.08

Activity Summary

IC50 2 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 2
CHEMBL4465
IC50 8.11 8.11 7.8 1
Sterol O-acyltransferase 1
CHEMBL2782
IC50 5.43 5.43 3730.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 9.0 hr Rattus norvegicus
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 = 7.8 nM 8.11 Inhibition of ACAT2 (unknown origin) 23711919
Sterol O-acyltransferase 1 IC50 = 3730.0 nM 5.43 Inhibition of ACAT1 (unknown origin) 23711919

Literature References

PubMed DOI Target Context # Activities
23711919 10.1016/j.bmcl.2013.04.075 Unchecked 1
23711919 10.1016/j.bmcl.2013.04.075 Sterol O-acyltransferase 2 1
23711919 10.1016/j.bmcl.2013.04.075 Sterol O-acyltransferase 1 1

Data from ChEMBL 36 via Core Engine