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Compound Detail

CHEMBL305602

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

Basic Information

ChEMBL ID CHEMBL305602
Phase Preclinical
Structure Type MOL
InChI Key VEKIKAXYTJSNHF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

546.0
MW (Da)
3.60
ALogP
9
HBA
2
HBD
152.5
PSA (Ų)
0.41
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20ClN3O7S3
MW 546.05
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.91

Activity Summary

IC50 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 10.0 10.0 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 636000.0 ng.hr.mL-1 Rattus norvegicus
Cmax 68308.76 nM Rattus norvegicus
T1/2 12.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.1 nM 10.0 Displacement of [125I]ET-1 from Endothelin A receptor 15055997

Literature References

PubMed DOI Target Context # Activities
15055997 10.1021/jm030528p Rattus norvegicus 5
15055997 10.1021/jm030528p Endothelin-1 receptor 2

Data from ChEMBL 36 via Core Engine