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Compound Detail

CHEMBL10589

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COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL10589
Phase Preclinical
Structure Type MOL
InChI Key SHTFYWSWZGSFTJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
3.84
ALogP
8
HBA
1
HBD
92.7
PSA (Ų)
0.51
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24O8
MW 476.48
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.55

Activity Summary

IC50 2 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 7.6 7.6 25.0 1
Endothelin receptor type B
CHEMBL1785
IC50 5.35 5.35 4500.0 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