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Compound Detail

CHEMBL316187

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COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL316187
Phase Preclinical
Structure Type MOL
InChI Key GJUNCAUBMKTRRC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

506.9
MW (Da)
5.29
ALogP
7
HBA
1
HBD
92.0
PSA (Ų)
0.35
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23ClN2O6
MW 506.94
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.74

Activity Summary

IC50 2 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL4631
IC50 8.01 8.01 9.7 1
Endothelin-1 receptor
CHEMBL4566
IC50 7.55 7.55 28.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11086733 10.1016/s0960-894x(00)00513-8 Endothelin-1 receptor 1
11086733 10.1016/s0960-894x(00)00513-8 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine