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Compound Detail

CHEMBL4519822

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CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1

Basic Information

ChEMBL ID CHEMBL4519822
Phase Preclinical
Structure Type MOL
InChI Key VNLAEVZRIYGZCY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
2.90
ALogP
11
HBA
2
HBD
146.7
PSA (Ų)
0.24
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26N6O6S2
MW 522.61
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.13

Activity Summary

IC50 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 8.85 8.85 1.4 1
Endothelin receptor type B
CHEMBL1785
IC50 7.05 7.05 90.0 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