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Compound Detail

CHEMBL417050

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COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL417050
Phase Preclinical
Structure Type MOL
InChI Key CFNXHTFSBOPIFW-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
4.44
ALogP
5
HBA
1
HBD
74.2
PSA (Ų)
0.70
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18O6
MW 402.40
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness 0.26

Activity Summary

IC50 3 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 7.07 7.07 86.0 2
Endothelin receptor type B
CHEMBL3949
IC50 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11985472 10.1021/jm010382z Endothelin-1 receptor 1
11985472 10.1021/jm010382z Endothelin receptor type B 1
11985472 10.1021/jm010382z Unchecked 1
15139753 10.1021/jm031041j Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine