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Compound Detail

CHEMBL424227

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CC[C@H](C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL424227
Phase Preclinical
Structure Type BOTH
InChI Key XPWGEIGKKBITIR-IEVKGZDRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

836.0
MW (Da)
3.01
ALogP
7
HBA
8
HBD
227.7
PSA (Ų)
0.07
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H57N7O8
MW 836.00
Aromatic Rings 4
Heavy Atoms 61
NP-Likeness -0.17

Activity Summary

IC50 1 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4130
IC50 6.82 6.82 150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 150.0 nM 6.82 Inhibition of endothelin (ET-A) binding to porcine heart membranes -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00349-X Endothelin-1 receptor 2

Data from ChEMBL 36 via Core Engine