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Compound Detail

CHEMBL133572

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Nc1c(S(=O)(=O)[O-])cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2S(=O)(=O)[O-])c2c1C(=O)c1ccccc1C2=O.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL133572
Phase Preclinical
Structure Type MOL
InChI Key MBOSUCSWTKOBGG-UHFFFAOYSA-L
Parent Compound CHEMBL1205686
Active Moiety CHEMBL1205686
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

637.4
MW (Da)
3.52
ALogP
12
HBA
5
HBD
231.6
PSA (Ų)
0.13
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H12Cl2N6Na2O8S2
MW 681.40
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 1
CHEMBL2530
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 1 IC50 = 1600.0 nM 5.8 The compound was evaluated for antagonist activity against P2X purinoceptor 1 (P... 12213051

Literature References

PubMed DOI Target Context # Activities
12213051 10.1021/jm020046y P2Y purinoceptor 1 1
12213051 10.1021/jm020046y P2X purinoceptor 1 1

Data from ChEMBL 36 via Core Engine