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Compound Detail

CHEMBL4521348

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CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1

Basic Information

ChEMBL ID CHEMBL4521348
Phase Preclinical
Structure Type MOL
InChI Key ZWTAXWXITAZUQP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

553.4
MW (Da)
3.21
ALogP
9
HBA
2
HBD
137.4
PSA (Ų)
0.31
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25BrN6O5S
MW 553.44
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 9.3 9.3 0.5 1
Endothelin receptor type B
CHEMBL1785
IC50 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27321813 10.1016/j.bmcl.2016.06.014 Endothelin-1 receptor 1
27321813 10.1016/j.bmcl.2016.06.014 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine