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Compound Detail

CHEMBL3898848

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CC(=O)O[C@H]1C[C@H]2[C@](C)(COC(=O)C(C)C)[C@@H](OC(=O)C(C)C)CC[C@]2(C)[C@H]2[C@@H](O)c3c(cc(-c4cccnc4)oc3=O)O[C@]12C

Basic Information

ChEMBL ID CHEMBL3898848
Phase Preclinical
Structure Type MOL
InChI Key KXSZDCQGXVFRNJ-VRKOFYPXSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
0
Publications
0
Known Names

Molecular Properties

639.7
MW (Da)
5.03
ALogP
11
HBA
1
HBD
151.5
PSA (Ų)
0.32
QED
3
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H45NO10
MW 639.74
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness 1.89

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 2
CHEMBL2653
IC50 9.3 9.3 0.5 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 = 0.5 nM 9.3 Inhibition of ACAT2 in mouse hepatic microsome membranes using [1-14C]oleoyl coe... -

Data from ChEMBL 36 via Core Engine