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Compound Detail

CHEMBL297107

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Cc1noc(NS(=O)(=O)c2ccsc2C(N)=O)c1Br

Basic Information

ChEMBL ID CHEMBL297107
Phase Preclinical
Structure Type MOL
InChI Key FSUWQETZHKACGA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

366.2
MW (Da)
1.71
ALogP
6
HBA
2
HBD
115.3
PSA (Ų)
0.85
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H8BrN3O4S2
MW 366.22
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -2.31

Activity Summary

IC50 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 6.08 6.08 838.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 838.0 nM 6.08 In vitro inhibition of endothelin binding to human Endothelin A receptor using [... 9171877

Literature References

PubMed DOI Target Context # Activities
9171877 10.1021/jm9608366 Endothelin-1 receptor 1
9171877 10.1021/jm9608366 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine