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Compound Detail

CHEMBL463559

MELAMPODIN A
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C=C1C(=O)O[C@@H]2/C=C(\C)[C@@H]3O[C@@H]3/C=C(/C(=O)OC)[C@H](O)[C@@H](OC(=O)[C@]3(C)O[C@@H]3C)[C@@H]12

Basic Information

ChEMBL ID CHEMBL463559
Name MELAMPODIN A
Phase Preclinical
Structure Type MOL
InChI Key ZFFQDPLDTMMAKO-PORRQQDQSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

420.4
MW (Da)
0.36
ALogP
9
HBA
1
HBD
124.2
PSA (Ų)
0.23
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C21H24O9
MW 420.41
Aromatic Rings 0
Heavy Atoms 30
NP-Likeness 2.86

Activity Summary

IC50 2 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 2
CHEMBL230
IC50 5.96 5.96 1100.0 1
Platelet
CHEMBL4296519
IC50 5.33 5.33 4680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin G/H synthase 2 IC50 = 1100.0 nM 5.96 Inhibition of COX2 16038536
Platelet IC50 = 4680.0 nM 5.33 Inhibition of serotonin release in bovine platelets 18271521

Literature References

PubMed DOI Target Context # Activities
27787995 10.1021/acs.jnatprod.6b00321 Mus musculus 2
18271521 10.1021/jm701318x Platelet 1
16038536 10.1021/np049655u Prostaglandin G/H synthase 2 1

Data from ChEMBL 36 via Core Engine