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Compound Detail

CHEMBL116705

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C=CCN(C)CCCCCCOc1ccc(C(=O)c2ccc(Br)cc2)c(NC)c1.O=C(O)/C=C/C(=O)O

Basic Information

ChEMBL ID CHEMBL116705
Phase Preclinical
Structure Type MOL
InChI Key LRBFTVIMFIJFQE-WLHGVMLRSA-N
Parent Compound CHEMBL611484
Active Moiety CHEMBL611484
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

459.4
MW (Da)
5.78
ALogP
4
HBA
1
HBD
41.6
PSA (Ų)
0.23
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H35BrN2O6
MW 575.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.89

Activity Summary

IC50 1 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lanosterol synthase
CHEMBL3593
IC50 8.39 8.39 4.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lanosterol synthase IC50 = 4.1 nM 8.39 In vitro inhibition of human 2,3-oxidosqualene cyclase. 12852766

Literature References

PubMed DOI Target Context # Activities
12852766 10.1021/jm021120f Lanosterol synthase 4

Data from ChEMBL 36 via Core Engine