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Compound Detail

CHEMBL3039411

BUSSEIN
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COC(=O)C[C@H]1C2(C)CC34OC5(C)O[C@@]6([C@H](OC(C)=O)C(OC(C)=O)[C@]7(C)C(/C(=C(/O)C(C)C)C(=O)O[C@H]7c7ccoc7)[C@@]6(O5)[C@H](OC(C)=O)[C@@]3(O)C2OC(=O)C(C)C)[C@]14C

Basic Information

ChEMBL ID CHEMBL3039411
Name BUSSEIN
Phase Preclinical
Structure Type MOL
InChI Key KVAGRMDUXLYLAZ-ZGZXWHTRSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

858.9
MW (Da)
3.67
ALogP
18
HBA
2
HBD
239.1
PSA (Ų)
0.16
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C43H54O18
MW 858.89
Aromatic Rings 1
Heavy Atoms 61
NP-Likeness 1.86

Activity Summary

IC50 2 meas. best 6.16
Ki 2 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Solute carrier organic anion transporter family member 1B1
CHEMBL1697668
Ki 6.42 6.42 380.0 1
Solute carrier organic anion transporter family member 1B3
CHEMBL1743121
Ki 6.28 6.28 530.0 1
Solute carrier organic anion transporter family member 1B1
CHEMBL1697668
IC50 6.16 6.16 691.8 1
Solute carrier organic anion transporter family member 1B3
CHEMBL1743121
IC50 6.16 6.16 691.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B3 3
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B1 3

Data from ChEMBL 36 via Core Engine