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Compound Detail

CHEMBL87252

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

Basic Information

ChEMBL ID CHEMBL87252
Phase Preclinical
Structure Type BOTH
InChI Key MFRKVXMTBRZSQE-MFNJSQIASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

806.0
MW (Da)
2.40
ALogP
8
HBA
9
HBD
261.9
PSA (Ų)
0.07
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 C42H59N7O9
MW 805.97
Aromatic Rings 3
Heavy Atoms 58
NP-Likeness 0.17

Activity Summary

IC50 1 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL4631
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin receptor type B IC50 = 2600.0 nM 5.58 Effective concentration against Endothelin B receptor from rat cerebellum 8410970

Literature References

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

Data from ChEMBL 36 via Core Engine