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Compound Detail

CHEMBL11369

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COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C

Basic Information

ChEMBL ID CHEMBL11369
Phase Preclinical
Structure Type MOL
InChI Key UTGRGVUJLJJKSH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

520.5
MW (Da)
4.16
ALogP
9
HBA
1
HBD
101.9
PSA (Ų)
0.44
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28O9
MW 520.53
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness 0.48

Activity Summary

IC50 2 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 9.3 9.3 0.5 1
Endothelin receptor type B
CHEMBL1785
IC50 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9089328 10.1021/jm9606507 Endothelin-1 receptor 1
9089328 10.1021/jm9606507 Endothelin receptor type B 1
9089328 10.1021/jm9606507 Endothelin receptor, ET-A/ET-B 1

Data from ChEMBL 36 via Core Engine