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Compound Detail

CHEMBL143820

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C[C@@H](CC(=O)O)CC(=O)N[C@@H](C)[C@H](/C=C/c1ccc2ccccc2c1)Cc1ccc(Cl)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL143820
Phase Preclinical
Structure Type MOL
InChI Key LVRZMZFXRFKCCY-KSYFVSBMSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

498.4
MW (Da)
7.02
ALogP
2
HBA
2
HBD
66.4
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29Cl2NO3
MW 498.45
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.02

Activity Summary

IC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene synthase
CHEMBL3338
IC50 8.6 8.6 2.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 54000.0 ng.hr.mL-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene synthase IC50 = 2.5 nM 8.6 Inhibitory activity against squalene synthase (SQS) obtained from HepG2 cells -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00033-9 Squalene synthase 1
- 10.1016/0960-894X(96)00033-9 Canis familiaris 1

Data from ChEMBL 36 via Core Engine