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Compound Detail

CHEMBL279471

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Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N

Basic Information

ChEMBL ID CHEMBL279471
Phase Preclinical
Structure Type MOL
InChI Key FMDCKBXKOAWRPM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
8
Publications
0
Known Names

Molecular Properties

458.6
MW (Da)
4.40
ALogP
7
HBA
2
HBD
125.1
PSA (Ų)
0.56
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N4O4S2
MW 458.57
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -2.02

Activity Summary

IC50 1 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 9.77 9.77 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 45800.0 ng.hr.mL-1 -
Cmax 28349.0 nM Rattus norvegicus
T1/2 1.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.17 nM 9.77 Inhibitory concentration was determined against selective Endothelin A receptor 11312921

Literature References

PubMed DOI Target Context # Activities
10579813 10.1021/jm9900063 Rattus norvegicus 2
11312921 10.1021/jm000349x Endothelin-1 receptor 1
11312921 10.1021/jm000349x Endothelin receptor, ET-A/ET-B 1
11312921 10.1021/jm000349x Rattus norvegicus 1
11312921 10.1021/jm000349x ADMET 1
10579813 10.1021/jm9900063 Endothelin-1 receptor 1
10579813 10.1021/jm9900063 Endothelin receptor, ET-A/ET-B 1
10579813 10.1021/jm9900063 No relevant target 1

Data from ChEMBL 36 via Core Engine