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Compound Detail

CHEMBL131271

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Nc1c(S(=O)(=O)[O-])cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)c(S(=O)(=O)[O-])c2)c2c1C(=O)c1ccccc1C2=O.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL131271
Phase Preclinical
Structure Type MOL
InChI Key PBDJUADDYHDIFK-UHFFFAOYSA-L
Parent Compound CHEMBL1205665
Active Moiety CHEMBL1205665
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
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 -0.51

Activity Summary

IC50 2 meas. best 5.94
Ki 1 meas. best 5.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 2
CHEMBL2135
IC50 5.94 5.94 1160.0 1
P2Y purinoceptor 12
CHEMBL2001
Ki 5.61 5.61 2450.0 1
P2X purinoceptor 1
CHEMBL2530
IC50 5.06 5.06 8800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12213051 10.1021/jm020046y P2X purinoceptor 1 1
12213051 10.1021/jm020046y P2Y purinoceptor 1 1
19463000 10.1021/jm9003297 P2Y purinoceptor 12 1
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1
27522579 10.1016/j.bmc.2016.07.027 Unchecked 1

Data from ChEMBL 36 via Core Engine