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Compound Detail

CHEMBL305576

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CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2

Basic Information

ChEMBL ID CHEMBL305576
Phase Preclinical
Structure Type MOL
InChI Key IUHMIOAKWHUFKU-YINIXLNUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

531.6
MW (Da)
5.40
ALogP
6
HBA
2
HBD
115.2
PSA (Ų)
0.36
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H33NO7
MW 531.61
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness 0.34

Activity Summary

Ki 1 meas. best 10.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
Ki 10.47 10.47 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor Ki = 0.034 nM 10.47 Binding affinity towards Endothelin A receptor 15055997

Literature References

PubMed DOI Target Context # Activities
15055997 10.1021/jm030528p Rattus norvegicus 1
15055997 10.1021/jm030528p Endothelin-1 receptor 1
15055997 10.1021/jm030528p Endothelin receptor 1

Data from ChEMBL 36 via Core Engine