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Compound Detail

CHEMBL276018

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COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc([N+](=O)[O-])c2)cc1

Basic Information

ChEMBL ID CHEMBL276018
Phase Preclinical
Structure Type MOL
InChI Key ZLGDGRLTDMLDDP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

461.4
MW (Da)
3.73
ALogP
8
HBA
1
HBD
117.4
PSA (Ų)
0.34
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H19NO8
MW 461.43
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.02

Activity Summary

IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 7.16 7.16 70.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 70.0 nM 7.16 Binding affinity against human cloned endothelin A receptor expressed in LTK-cel... 9089328

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