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Compound Detail

CHEMBL524064

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Nc1c(S(=O)(=O)[O-])cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O.[Na+]

Basic Information

ChEMBL ID CHEMBL524064
Phase Preclinical
Structure Type MOL
InChI Key UQWUDXYPYWXKKT-UHFFFAOYSA-M
Parent Compound CHEMBL1208288
Active Moiety CHEMBL1208288
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
2.73
ALogP
7
HBA
4
HBD
163.9
PSA (Ų)
0.28
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H13N2NaO7S
MW 460.40
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.22

Activity Summary

IC50 2 meas. best 6.0
Ki 2 meas. best 5.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 2
CHEMBL2135
IC50 6.0 6.0 1000.0 1
P2Y purinoceptor 4
CHEMBL2123
IC50 5.21 5.21 6100.0 1
5'-nucleotidase
CHEMBL1075214
Ki 5.18 5.18 6530.0 1
P2Y purinoceptor 12
CHEMBL2001
Ki 4.6 4.6 25100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19463000 10.1021/jm9003297 P2Y purinoceptor 12 1
20146483 10.1021/jm901851t 5'-nucleotidase 1
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1
28306255 10.1021/acs.jmedchem.7b00030 P2Y purinoceptor 4 1

Data from ChEMBL 36 via Core Engine