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Compound Detail

CHEMBL273660

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COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)[O-])c2cc(OC)c3c(c2)OCO3)cc1.[Na+]

Basic Information

ChEMBL ID CHEMBL273660
Phase Preclinical
Structure Type MOL
InChI Key QTBXSWKNBOWQIN-QTXBERLJSA-M
Parent Compound CHEMBL369085
Active Moiety CHEMBL369085
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
4.40
ALogP
6
HBA
1
HBD
91.3
PSA (Ų)
0.41
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21NaO7
MW 468.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness 0.18

Activity Summary

IC50 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 8.0 8.0 10.0 1
Endothelin receptor type B
CHEMBL1785
IC50 4.8 4.8 15700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9089328 10.1021/jm9606507 Endothelin-1 receptor 2
9089328 10.1021/jm9606507 Endothelin receptor type B 1
9089328 10.1021/jm9606507 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine