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Compound Detail

CHEMBL271673

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

Basic Information

ChEMBL ID CHEMBL271673
Phase Preclinical
Structure Type MOL
InChI Key KINIBOSGQKLOIT-UHFFFAOYSA-M
Parent Compound CHEMBL1206416
Active Moiety CHEMBL1206416
9
Targets
12
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

428.9
MW (Da)
3.69
ALogP
6
HBA
3
HBD
126.6
PSA (Ų)
0.34
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H12ClN2NaO5S
MW 450.83
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.49

Activity Summary

IC50 6 meas. best 6.0
Ki 6 meas. best 5.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.0 5.73 990.0 2
P2Y purinoceptor 4
CHEMBL2123
IC50 5.52 5.52 3030.0 1
5'-nucleotidase
CHEMBL1075214
Ki 5.32 5.32 4810.0 1
P2Y purinoceptor 2
CHEMBL4398
IC50 5.28 5.28 5310.0 1
P2Y purinoceptor 12
CHEMBL2001
Ki 5.13 5.13 7350.0 1
Unchecked
CHEMBL612545
Ki 4.91 4.85 12400.0 2
Ectonucleoside triphosphate diphosphohydrolase 1
CHEMBL2767
Ki 4.8 4.8 15700.0 1
Ectonucleoside triphosphate diphosphohydrolase 2
CHEMBL3300
Ki 4.75 4.75 18000.0 1
Unchecked
CHEMBL612545
IC50 4.75 4.75 17600.0 1
P2Y purinoceptor 2
CHEMBL1075298
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 990.0 nM 6.0 Inhibition of 8-((4-chlorophenyl)amino)naphthalene-1-sulfonic acid binding to CD... 36701569
P2Y purinoceptor 4 IC50 = 3030.0 nM 5.52 Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells ass... 28306255
Cyclin-dependent kinase 2 IC50 = 3490.0 nM 5.46 Inhibition of 8-((4-chlorophenyl)amino)naphthalene-1-sulfonic acid binding to CD... 36701569
5'-nucleotidase Ki = 4810.0 nM 5.32 Inhibition of rat ecto-5'-nucleotidase expressed in Sf9 cells by capillary elect... 20146483
P2Y purinoceptor 2 IC50 = 5310.0 nM 5.28 Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed ... 18006312
P2Y purinoceptor 12 Ki = 7350.0 nM 5.13 Displacement of [3H]PSB0413 from human platelet P2Y12 receptor 19463000
Unchecked Ki = 12400.0 nM 4.91 Inhibition of recombinant Legionella pneumophila 130b His6-tagged NTPDase (41 to... 27522579
Ectonucleoside triphosphate diphosphohydrolase 1 Ki = 15700.0 nM 4.8 Inhibition of rat CD39 expressed in CHO cells using ATP as substrate incubated f... 32786396
Unchecked Ki = 16400.0 nM 4.79 Inhibition of rat NTPDase3 expressed in CHO cells using ATP as substrate incubat... 32786396
Unchecked IC50 = 17600.0 nM 4.75 Inhibition of recombinant Legionella pneumophila 130b His6-tagged NTPDase (41 to... 27522579
Ectonucleoside triphosphate diphosphohydrolase 2 Ki = 18000.0 nM 4.75 Inhibition of rat NTPDase2 expressed in CHO cells using ATP as substrate incubat... 32786396
P2Y purinoceptor 2 IC50 = 20000.0 nM 4.7 Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as i... 18006312

Literature References

PubMed DOI Target Context # Activities
19463000 10.1021/jm9003297 NON-PROTEIN TARGET 6
27522579 10.1016/j.bmc.2016.07.027 Unchecked 3
36701569 10.1021/acs.jmedchem.2c01731 Cyclin-dependent kinase 2 3
18006312 10.1016/j.bmcl.2007.10.082 P2Y purinoceptor 2 2
19463000 10.1021/jm9003297 P2Y purinoceptor 12 1
20146483 10.1021/jm901851t 5'-nucleotidase 1
28306255 10.1021/acs.jmedchem.7b00030 P2Y purinoceptor 4 1
32786396 10.1021/acs.jmedchem.0c01044 Ectonucleoside triphosphate diphosphohydrolase 1 1
32786396 10.1021/acs.jmedchem.0c01044 Ectonucleoside triphosphate diphosphohydrolase 2 1
32786396 10.1021/acs.jmedchem.0c01044 Unchecked 1

Data from ChEMBL 36 via Core Engine