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Compound Detail

CHEMBL340190

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CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1

Basic Information

ChEMBL ID CHEMBL340190
Phase Preclinical
Structure Type MOL
InChI Key HZYXDFYJDODHTN-UIFDUCBYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

516.6
MW (Da)
4.96
ALogP
5
HBA
1
HBD
79.3
PSA (Ų)
0.45
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34F2N2O5
MW 516.59
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.72

Activity Summary

IC50 2 meas. best 8.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 8.86 8.86 1.4 1
Endothelin receptor type B
CHEMBL1785
IC50 5.98 5.98 1040.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11689084 10.1021/jm010237l Endothelin-1 receptor 1
11689084 10.1021/jm010237l Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine