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Compound Detail

CHEMBL302493

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COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCOCC3)c2)cc1

Basic Information

ChEMBL ID CHEMBL302493
Phase Preclinical
Structure Type MOL
InChI Key OEMNPEMEFUYQJO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

559.6
MW (Da)
3.92
ALogP
9
HBA
1
HBD
95.9
PSA (Ų)
0.29
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H33NO8
MW 559.62
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.23

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 2.0 nM 8.7 Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor. 10377221

Literature References

PubMed DOI Target Context # Activities
10377221 10.1021/jm980504w Endothelin-1 receptor 1
10377221 10.1021/jm980504w Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine