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Compound Detail

CHEMBL48120

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Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL48120
Phase Preclinical
Structure Type MOL
InChI Key QPYKESGJRJWVKI-UHFFFAOYSA-N
Parent Compound CHEMBL1178890
Active Moiety CHEMBL1178890
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

402.8
MW (Da)
3.05
ALogP
8
HBA
2
HBD
127.3
PSA (Ų)
0.67
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 C15H12ClF3N4O7S2
MW 516.86
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -2.65

Activity Summary

IC50 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 7.24 7.24 57.0 1
Endothelin receptor type B
CHEMBL1785
IC50 4.04 4.04 92100.0 1

Activity Data Samples

Top measurements by pChEMBL value

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