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Compound Detail

CHEMBL4171883

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COc1cc([C@@H]2Oc3c(OC)cc(/C=C/COC(=O)CC(C)C)cc3[C@H]2COC(=O)CC(C)C)ccc1O

Basic Information

ChEMBL ID CHEMBL4171883
Phase Preclinical
Structure Type MOL
InChI Key HZUKVQHPHZPOEM-PLVUCCGMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

526.6
MW (Da)
5.82
ALogP
8
HBA
1
HBD
100.5
PSA (Ų)
0.35
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C30H38O8
MW 526.63
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness 1.33

Activity Summary

IC50 1 meas. best 4.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma congolense
CHEMBL4296607
IC50 4.87 4.87 13400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma congolense IC50 = 13400.0 nM 4.87 Trypanocidal activity against bloodstream form of Trypanosoma congolense IL3000 ... 30896183

Literature References

PubMed DOI Target Context # Activities
29738243 10.1021/acs.jnatprod.8b00135 Plasmodium falciparum 1
29738243 10.1021/acs.jnatprod.8b00135 A2780 1
30896183 10.1021/acs.jnatprod.8b00670 Trypanosoma congolense 1

Data from ChEMBL 36 via Core Engine