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Compound Detail

CHEMBL19921

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Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O

Basic Information

ChEMBL ID CHEMBL19921
Phase Preclinical
Structure Type MOL
InChI Key YHVRYVBITHJKNK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
8
Publications
0
Known Names

Molecular Properties

455.0
MW (Da)
4.55
ALogP
7
HBA
2
HBD
109.5
PSA (Ų)
0.53
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 C19H19ClN2O5S2
MW 454.96
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.22

Activity Summary

IC50 1 meas. best 9.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 9.85 9.85 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 15800.0 ng.hr.mL-1 -
Cmax 5714.79 nM Rattus norvegicus
T1/2 3.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.14 nM 9.85 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