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Compound Detail

CHEMBL299921

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Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1

Basic Information

ChEMBL ID CHEMBL299921
Phase Preclinical
Structure Type MOL
InChI Key WIDWAOUINOXRGU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

493.0
MW (Da)
5.02
ALogP
8
HBA
2
HBD
127.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17ClN4O5S2
MW 492.97
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.83

Activity Summary

IC50 1 meas. best 10.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 10.1 10.1 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 362500.0 ng.hr.mL-1 Rattus norvegicus
Cmax 133882.39 nM Rattus norvegicus
T1/2 5.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.08 nM 10.1 Displacement of [125I]ET-1 from Endothelin A receptor 15055997

Literature References

PubMed DOI Target Context # Activities
15055997 10.1021/jm030528p Rattus norvegicus 3
15055997 10.1021/jm030528p Endothelin-1 receptor 2

Data from ChEMBL 36 via Core Engine