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Compound Detail

CHEMBL10635

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COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1

Basic Information

ChEMBL ID CHEMBL10635
Phase Preclinical
Structure Type MOL
InChI Key LVGJFPBFENMSKI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

474.5
MW (Da)
3.59
ALogP
8
HBA
1
HBD
92.7
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22O8
MW 474.47
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.33

Activity Summary

IC50 2 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 8.12 8.12 7.5 1
Endothelin receptor type B
CHEMBL1785
IC50 5.8 5.8 1600.0 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

Data from ChEMBL 36 via Core Engine