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Compound Detail

CHEMBL2163722

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COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1

Basic Information

ChEMBL ID CHEMBL2163722
Phase Preclinical
Structure Type MOL
InChI Key BCPQODVHPDJJAT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

661.5
MW (Da)
2.73
ALogP
13
HBA
1
HBD
172.9
PSA (Ų)
0.22
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25BrN8O7S
MW 661.49
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.27

Activity Summary

IC50 2 meas. best 6.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 6.73 6.73 187.0 1
Endothelin receptor type B
CHEMBL1785
IC50 5.83 5.83 1474.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22862294 10.1021/jm3009103 Endothelin receptor type B 1
22862294 10.1021/jm3009103 Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine