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Compound Detail

CHEMBL29598

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Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C

Basic Information

ChEMBL ID CHEMBL29598
Phase Preclinical
Structure Type MOL
InChI Key QSDFLNIZMIGXOO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
4.99
ALogP
8
HBA
1
HBD
124.3
PSA (Ų)
0.35
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N4O5S
MW 476.51
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.03

Activity Summary

Ki 2 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
Ki 9.12 9.12 0.8 1
Endothelin receptor type B
CHEMBL1785
Ki 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12502366 10.1021/jm020289q Endothelin-1 receptor 1
12502366 10.1021/jm020289q Oryctolagus cuniculus 1
12502366 10.1021/jm020289q Endothelin receptor type B 1
12502366 10.1021/jm020289q Homo sapiens 1

Data from ChEMBL 36 via Core Engine