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Compound Detail

CHEMBL277447

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Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNC(=O)CC(C)(C)C)c1C

Basic Information

ChEMBL ID CHEMBL277447
Phase Preclinical
Structure Type MOL
InChI Key GBHZRMWZYDRRRK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
5.47
ALogP
7
HBA
2
HBD
127.3
PSA (Ų)
0.31
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N4O5S
MW 522.63
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.33

Activity Summary

Ki 1 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
Ki 11.0 11.0 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 100.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor Ki = 0.01 nM 11.0 Inhibitory concentration against Endothelin A receptor 14998318

Literature References

PubMed DOI Target Context # Activities
14998318 10.1021/jm030480f Rattus norvegicus 2
14998318 10.1021/jm030480f Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine