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Compound Detail

CHEMBL137671

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CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O

Basic Information

ChEMBL ID CHEMBL137671
Phase Preclinical
Structure Type BOTH
InChI Key NFYJYRSYGSKRRZ-XRKIENNPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

669.8
MW (Da)
-0.62
ALogP
7
HBA
9
HBD
263.0
PSA (Ų)
0.08
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H47N9O7
MW 669.78
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness 1.01

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 The compound was tested for binding inhibitory activity against Endothelin A rec... 7473559

Literature References

PubMed DOI Target Context # Activities
7473559 10.1021/jm00021a021 Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine