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Compound Detail

CHEMBL262166

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CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL262166
Phase Preclinical
Structure Type BOTH
InChI Key POTOCBRVVBLKOB-BZFYIXCDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

864.0
MW (Da)
1.40
ALogP
9
HBA
10
HBD
302.3
PSA (Ų)
0.06
QED
2
Ro5 Violations
25
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H57N7O12
MW 863.97
Aromatic Rings 3
Heavy Atoms 62
NP-Likeness 0.14

Activity Summary

IC50 1 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor
CHEMBL2111453
IC50 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin receptor IC50 = 5200.0 nM 5.28 Binding affinity against Endothelin receptor from rat heart ventricle 8410970

Literature References

PubMed DOI Target Context # Activities
8410970 10.1021/jm00070a001 Endothelin receptor 1

Data from ChEMBL 36 via Core Engine