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Compound Detail

CHEMBL446979

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O=C(O[C@@H]1O[C@@H]2COC(=O)c3cc(O)c(O)c(O)c3-c3c(cc(O)c(O)c3O)C(=O)O[C@H]2[C@@H]2OC(=O)c3cc(O)c(O)c(O)c3-c3c(cc(O)c(O)c3O)C(=O)O[C@@H]12)c1cc(O)c(O)c(O)c1

Basic Information

ChEMBL ID CHEMBL446979
Phase Preclinical
Structure Type MOL
InChI Key SWRFKGRMQVLMKA-JIZJWZDPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

936.6
MW (Da)
1.65
ALogP
26
HBA
15
HBD
444.2
PSA (Ų)
0.07
QED
3
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C41H28O26
MW 936.65
Aromatic Rings 5
Heavy Atoms 67
NP-Likeness 0.90

Activity Summary

IC50 1 meas. best 5.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene monooxygenase
CHEMBL4241
IC50 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene monooxygenase IC50 = 7000.0 nM 5.16 Inhibition of C-terminal hexahistidine-tagged rat recombinant squalene epoxidase... 11520216

Literature References

PubMed DOI Target Context # Activities
30497912 10.1016/j.bmcl.2018.11.042 HT-22 6
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
30497912 10.1016/j.bmcl.2018.11.042 No relevant target 1
30497912 10.1016/j.bmcl.2018.11.042 Mitogen-activated protein kinase 1 and 3 (ERK2 and ERK1) 1
30497912 10.1016/j.bmcl.2018.11.042 Unchecked 1
30497912 10.1016/j.bmcl.2018.11.042 MAP kinase p38 1

Data from ChEMBL 36 via Core Engine