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Compound Detail

CHEMBL52338

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COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)[O-])c2ccc3nsnc3c2)cc1.[Na+]

Basic Information

ChEMBL ID CHEMBL52338
Phase Preclinical
Structure Type MOL
InChI Key DXIOGBZFNYYYCJ-SIZUISDESA-M
Parent Compound CHEMBL1205104
Active Moiety CHEMBL1205104
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

502.6
MW (Da)
5.84
ALogP
7
HBA
1
HBD
98.6
PSA (Ų)
0.24
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25N2NaO5S
MW 524.57
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.57

Activity Summary

IC50 2 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 6.24 6.24 580.0 1
Endothelin receptor type B
CHEMBL3949
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9873432 10.1016/s0960-894x(98)00301-1 Endothelin-1 receptor 1
9873432 10.1016/s0960-894x(98)00301-1 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine