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Compound Detail

CHEMBL496030

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

Basic Information

ChEMBL ID CHEMBL496030
Phase Preclinical
Structure Type MOL
InChI Key VLZVLXBAUVQEKH-UHFFFAOYSA-M
Parent Compound CHEMBL1208092
Active Moiety CHEMBL1208092
8
Targets
12
Activities
2
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

410.4
MW (Da)
2.74
ALogP
7
HBA
4
HBD
146.8
PSA (Ų)
0.23
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 C20H13N2NaO6S
MW 432.39
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.11

Activity Summary

IC50 8 meas. best 6.23
Ki 4 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 2
CHEMBL2135
IC50 6.23 6.23 588.0 1
5'-nucleotidase
CHEMBL1075214
Ki 6.21 6.21 620.0 1
P2Y purinoceptor 4
CHEMBL2123
IC50 5.65 5.59 2220.0 3
P2Y purinoceptor 2
CHEMBL4398
IC50 5.33 5.33 4630.0 2
P2Y purinoceptor 6
CHEMBL3543
IC50 5.28 5.28 5300.0 1
P2Y purinoceptor 6
CHEMBL4714
IC50 5.28 5.28 5300.0 1
P2Y purinoceptor 12
CHEMBL2001
Ki 5.0 5.0 10000.0 2
Ectonucleoside triphosphate diphosphohydrolase 1
CHEMBL5722
Ki 4.97 4.97 10700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 2 IC50 = 588.0 nM 6.23 Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte... 21207957
5'-nucleotidase Ki = 620.0 nM 6.21 Inhibition of rat ecto-5'-nucleotidase expressed in Sf9 cells by capillary elect... 20146483
P2Y purinoceptor 4 IC50 = 2220.0 nM 5.65 Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma ... 21207957
P2Y purinoceptor 4 IC50 = 2370.0 nM 5.62 Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assess... 20146483
P2Y purinoceptor 4 IC50 = 3160.0 nM 5.5 Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells ass... 28306255
P2Y purinoceptor 2 IC50 = 4630.0 nM 5.33 Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assess... 20146483
P2Y purinoceptor 2 IC50 = 4630.0 nM 5.33 Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma ... 21207957
P2Y purinoceptor 6 IC50 = 5300.0 nM 5.28 Antagonist activity at rat P2Y6 receptor expressed in astrocytoma cells assessed... 20146483
P2Y purinoceptor 6 IC50 = 5300.0 nM 5.28 Antagonist activity against human P2Y6 receptor expressed in 1321N1 astrocytoma ... 21207957
P2Y purinoceptor 12 Ki = 10000.0 nM 5.0 Displacement of [3H]PSB0413 from human platelet P2Y12 receptor 19463000
P2Y purinoceptor 12 Ki = 10000.0 nM 5.0 Displacement of [3H]PSB0413 from human platelet P2Y12 receptor 21207957
Ectonucleoside triphosphate diphosphohydrolase 1 Ki = 10700.0 nM 4.97 Inhibition of human NTPdase1 by capillary electrophoresis method 20146483

Literature References

PubMed DOI Target Context # Activities
19463000 10.1021/jm9003297 P2Y purinoceptor 12 2
20146483 10.1021/jm901851t 5'-nucleotidase 1
20146483 10.1021/jm901851t P2Y purinoceptor 2 1
20146483 10.1021/jm901851t P2Y purinoceptor 4 1
20146483 10.1021/jm901851t P2Y purinoceptor 6 1
20146483 10.1021/jm901851t Ectonucleoside triphosphate diphosphohydrolase 1 1
20146483 10.1021/jm901851t Ectonucleoside triphosphate diphosphohydrolase 2 1
20146483 10.1021/jm901851t Nucleoside triphosphate diphosphohydrolase 3 1
20146483 10.1021/jm901851t Ectonucleoside triphosphate diphosphohydrolase 3 1
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1
21207957 10.1021/jm1012193 P2Y purinoceptor 2 1
21207957 10.1021/jm1012193 P2Y purinoceptor 4 1
21207957 10.1021/jm1012193 P2Y purinoceptor 6 1
21207957 10.1021/jm1012193 P2Y purinoceptor 12 1
28306255 10.1021/acs.jmedchem.7b00030 P2Y purinoceptor 4 1

Data from ChEMBL 36 via Core Engine