Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL444545

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCCC(=O)O)c1

Basic Information

ChEMBL ID CHEMBL444545
Phase Preclinical
Structure Type MOL
InChI Key CXPJVEDWFYFWNH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

492.4
MW (Da)
4.52
ALogP
7
HBA
1
HBD
92.0
PSA (Ų)
0.42
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23F3N2O6
MW 492.45
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 4.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 4.19 4.19 64000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 64000.0 nM 4.19 In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ... 10890162

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

Data from ChEMBL 36 via Core Engine