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Compound Detail

CHEMBL597591

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Nc1c(S(=O)(=O)[O-])cc(Nc2ccc(CC(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O.[Na+]

Basic Information

ChEMBL ID CHEMBL597591
Phase Preclinical
Structure Type MOL
InChI Key MQQNDKIVRDZQRS-UHFFFAOYSA-M
Parent Compound CHEMBL1208440
Active Moiety CHEMBL1208440
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
2.66
ALogP
7
HBA
4
HBD
163.9
PSA (Ų)
0.26
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 C22H15N2NaO7S
MW 474.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.25

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 2
CHEMBL2135
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 2 IC50 = 1000.0 nM 6.0 Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte... 21207957

Literature References

PubMed DOI Target Context # Activities
20146483 10.1021/jm901851t 5'-nucleotidase 1
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1

Data from ChEMBL 36 via Core Engine