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Compound Detail

CHEMBL26474

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COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL26474
Phase Preclinical
Structure Type MOL
InChI Key FGOULBWWTIMGSP-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

476.9
MW (Da)
5.28
ALogP
6
HBA
1
HBD
82.8
PSA (Ų)
0.39
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21ClN2O5
MW 476.92
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.94

Activity Summary

IC50 4 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 7.75 7.75 18.0 2
Endothelin receptor type B
CHEMBL4631
IC50 7.47 7.47 34.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10890162 10.1016/s0960-894x(00)00232-8 Endothelin-1 receptor 1
10890162 10.1016/s0960-894x(00)00232-8 Endothelin receptor type B 1
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