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Compound Detail

CHEMBL300000

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CCOc1ccc2c(c1)[C@@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2

Basic Information

ChEMBL ID CHEMBL300000
Phase Preclinical
Structure Type MOL
InChI Key PBTQECKJFWIROQ-KAYWLYCHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

521.5
MW (Da)
3.87
ALogP
8
HBA
2
HBD
124.0
PSA (Ų)
0.41
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 C28H27NO9
MW 521.52
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.28

Activity Summary

IC50 1 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 7.07 7.07 85.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11425549 10.1016/s0960-894x(01)00273-6 Endothelin-1 receptor 1
11425549 10.1016/s0960-894x(01)00273-6 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine