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Compound Detail

CHEMBL48031

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Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1

Basic Information

ChEMBL ID CHEMBL48031
Phase Preclinical
Structure Type MOL
InChI Key JWLWWTTYSPSXMJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

456.3
MW (Da)
4.17
ALogP
6
HBA
2
HBD
101.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14BrN3O4S2
MW 456.34
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -2.48

Activity Summary

IC50 2 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 6.98 6.98 104.0 1
Endothelin receptor type B
CHEMBL1785
IC50 4.17 4.17 67400.0 1

Activity Data Samples

Top measurements by pChEMBL value

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