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Compound Detail

CHEMBL4538570

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CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1

Basic Information

ChEMBL ID CHEMBL4538570
Phase Preclinical
Structure Type MOL
InChI Key KZURRFQRQGCFPT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

607.8
MW (Da)
6.43
ALogP
10
HBA
1
HBD
116.2
PSA (Ų)
0.14
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29N5O4S3
MW 607.78
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 10.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 10.59 10.59 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.026 nM 10.59 Displacement of 125I-ET1 from ETA receptor in rat A7R5 cells 27321813

Literature References

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

Data from ChEMBL 36 via Core Engine