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Compound Detail

CHEMBL1791277

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

Basic Information

ChEMBL ID CHEMBL1791277
Phase Preclinical
Structure Type BOTH
InChI Key FFHBVWCUKLBZIM-ISNUVAIJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

839.9
MW (Da)
-0.27
ALogP
10
HBA
11
HBD
331.0
PSA (Ų)
0.06
QED
2
Ro5 Violations
24
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H53N9O12
MW 839.90
Aromatic Rings 3
Heavy Atoms 60
NP-Likeness 0.08

Activity Summary

IC50 1 meas. best 4.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL4631
IC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin receptor type B IC50 = 14000.0 nM 4.85 Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) ... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00152-J Endothelin-1 receptor 1
- 10.1016/0960-894X(95)00152-J Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine