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Compound Detail

CHEMBL295632

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COC(=O)c1cc(OC)cc(OC)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl

Basic Information

ChEMBL ID CHEMBL295632
Phase Preclinical
Structure Type MOL
InChI Key WGQYSLYCRPURSK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

516.0
MW (Da)
3.55
ALogP
10
HBA
2
HBD
146.1
PSA (Ų)
0.43
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 C19H18ClN3O8S2
MW 515.95
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 6.26 6.26 549.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 549.0 nM 6.26 In vitro inhibition of endothelin binding to human Endothelin A receptor using [... 9171877

Literature References

PubMed DOI Target Context # Activities
9171877 10.1021/jm9608366 Endothelin-1 receptor 1
9171877 10.1021/jm9608366 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine