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Compound Detail

CHEMBL307324

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CC(C)C[C@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(C)C)C(=O)N1C

Basic Information

ChEMBL ID CHEMBL307324
Phase Preclinical
Structure Type BOTH
InChI Key DAFCCKSWJXSKCS-HOIWYFOJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

624.7
MW (Da)
1.17
ALogP
6
HBA
5
HBD
181.0
PSA (Ų)
0.31
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H44N6O7
MW 624.74
Aromatic Rings 2
Heavy Atoms 45
NP-Likeness 1.01

Activity Summary

IC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4130
IC50 7.46 7.46 35.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 35.0 nM 7.46 Binding activity against Endothelin A receptor of Porcine aortic smooth muscle m... 1317926

Literature References

PubMed DOI Target Context # Activities
1317926 10.1021/jm00089a028 Endothelin-1 receptor 1
1317926 10.1021/jm00089a028 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine