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Compound Detail

CHEMBL481811

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C=CCN(C)C/C=C/COc1ccc2c(-c3ccc(Br)cc3)coc2c1.O=C(O)/C=C/C(=O)O

Basic Information

ChEMBL ID CHEMBL481811
Phase Preclinical
Structure Type MOL
InChI Key SMELXZLWDUMFEA-FREMDOHUSA-N
Parent Compound CHEMBL65553
Active Moiety CHEMBL65553
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

412.3
MW (Da)
5.92
ALogP
3
HBA
0
HBD
25.6
PSA (Ų)
0.43
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26BrNO6
MW 528.40
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.26

Activity Summary

IC50 5 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lanosterol synthase ERG7
CHEMBL5355
IC50 6.68 6.68 210.0 1
Unchecked
CHEMBL612545
IC50 5.92 5.72 1200.0 2
Cycloartenol synthase
CHEMBL5356
IC50 5.52 5.52 3000.0 1
Lanosterol synthase
CHEMBL3593
IC50 4.05 4.05 90000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19119009 10.1016/j.bmcl.2008.12.040 Unchecked 3
19119009 10.1016/j.bmcl.2008.12.040 Lanosterol synthase ERG7 1
19119009 10.1016/j.bmcl.2008.12.040 Cycloartenol synthase 1
19119009 10.1016/j.bmcl.2008.12.040 Lanosterol synthase 1

Data from ChEMBL 36 via Core Engine