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Compound Detail

CHEMBL62159

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Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C

Basic Information

ChEMBL ID CHEMBL62159
Phase Preclinical
Structure Type MOL
InChI Key JOBUYXCZCOHOSS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

465.0
MW (Da)
4.55
ALogP
7
HBA
2
HBD
125.1
PSA (Ų)
0.57
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17ClN4O4S2
MW 464.96
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -2.14

Activity Summary

IC50 1 meas. best 10.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 10.3 10.3 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 373400.0 ng.hr.mL-1 Rattus norvegicus
Cmax 98288.02 nM Rattus norvegicus
T1/2 5.11 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.05 nM 10.3 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