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Compound Detail

CHEMBL34540

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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](N)Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC

Basic Information

ChEMBL ID CHEMBL34540
Phase Preclinical
Structure Type BOTH
InChI Key NTSBFTNRWQVBCA-IVGDYKFASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

795.9
MW (Da)
1.13
ALogP
9
HBA
10
HBD
290.6
PSA (Ų)
0.06
QED
2
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H57N9O9
MW 795.94
Aromatic Rings 3
Heavy Atoms 57
NP-Likeness 0.14

Activity Summary

IC50 1 meas. best 4.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 4.36 4.36 44000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 44000.0 nM 4.36 Compound was evaluated for the binding affinity to endothelin receptor in the ra... 1315867

Literature References

PubMed DOI Target Context # Activities
1324321 10.1021/jm00095a029 Endothelin-1 receptor 1
1324321 10.1021/jm00095a029 Endothelin receptor type B 1
1324321 10.1021/jm00095a029 Rattus norvegicus 1
- 10.1016/0960-894X(95)00152-J Endothelin-1 receptor 1
- 10.1016/0960-894X(95)00152-J Endothelin receptor type B 1
1315867 10.1021/jm00087a001 Endothelin-1 receptor 1
1315867 10.1021/jm00087a001 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine