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Compound Detail

CHEMBL458193

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O=C1O[C@H]2[C@H](O)[C@@H](CO)OC(O)[C@@H]2OC(=O)c2cc(O)c(O)c(O)c2-c2c1cc(O)c(O)c2O

Basic Information

ChEMBL ID CHEMBL458193
Phase Preclinical
Structure Type MOL
InChI Key GEAGRKQCZVLNAU-NNIZZFLASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

482.4
MW (Da)
-1.28
ALogP
14
HBA
9
HBD
243.9
PSA (Ų)
0.17
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C20H18O14
MW 482.35
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 1.71

Activity Summary

IC50 1 meas. best 4.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene monooxygenase
CHEMBL4241
IC50 4.5 4.5 32000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene monooxygenase IC50 = 32000.0 nM 4.5 Inhibition of C-terminal hexahistidine-tagged rat recombinant squalene epoxidase... 11520216

Literature References

PubMed DOI Target Context # Activities
9834152 10.1021/np9801458 Prothrombin 4
9834152 10.1021/np9801458 Plasma 3
11277742 10.1021/np000506v Pseudomonas fluorescens 1
11277742 10.1021/np000506v 5637 1
11277742 10.1021/np000506v Bacillus subtilis 1
11520216 10.1021/np010100y Squalene monooxygenase 1
1431932 10.1021/np50086a002 TE-671 1
1431932 10.1021/np50086a002 HCT-8 1
1431932 10.1021/np50086a002 A549 1
1431932 10.1021/np50086a002 KB 1
1431932 10.1021/np50086a002 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine