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Compound Detail

CHEMBL103501

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COc1ccc(C2(OC(=O)N[C@@H](C)c3ccccc3)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL103501
Phase Preclinical
Structure Type MOL
InChI Key AVTITURLDNGPIM-DAXAVGQISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

563.6
MW (Da)
6.32
ALogP
7
HBA
1
HBD
92.3
PSA (Ų)
0.25
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H29NO7
MW 563.61
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness 0.05

Activity Summary

IC50 1 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 18.0 nM 7.75 Binding affinity for human Endothelin A receptor expressed in LtK- cells -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00002-4 Endothelin-1 receptor 1
- 10.1016/S0960-894X(97)00002-4 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine