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Compound Detail

CHEMBL367017

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COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1

Basic Information

ChEMBL ID CHEMBL367017
Phase Preclinical
Structure Type MOL
InChI Key VICZNPBUMWESDN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

654.8
MW (Da)
4.26
ALogP
12
HBA
2
HBD
171.6
PSA (Ų)
0.17
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H26N6O7S3
MW 654.75
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -1.56

Activity Summary

IC50 2 meas. best 5.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 5.55 5.55 2838.0 1
Endothelin receptor type B
CHEMBL1785
IC50 5.43 5.43 3676.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12617928 10.1016/s0960-894x(02)01083-1 Endothelin-1 receptor 1
12617928 10.1016/s0960-894x(02)01083-1 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine