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Compound Detail

CHEMBL1672104

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

Basic Information

ChEMBL ID CHEMBL1672104
Phase Preclinical
Structure Type MOL
InChI Key DHHMYWVFMSHEIP-UHFFFAOYSA-L
Parent Compound CHEMBL1741102
Active Moiety CHEMBL1741102
8
Targets
13
Activities
2
Assay Types
0
PK Parameters
19
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 12 meas. best 8.28
Ki 1 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.28 8.1233 5.3 3
P2X purinoceptor 2
CHEMBL2135
IC50 7.1 6.67 79.0 2
P2X purinoceptor 1
CHEMBL2530
IC50 6.38 5.855 422.0 2
P2X purinoceptor 3
CHEMBL4824
IC50 6.31 6.31 494.0 1
P2X purinoceptor 2
CHEMBL2531
IC50 6.16 6.16 690.0 2
P2X2/P2X3 receptor
CHEMBL3137277
IC50 5.98 5.98 1042.0 1
P2Y purinoceptor 2
CHEMBL4398
IC50 5.0 5.0 10000.0 1
P2Y purinoceptor 12
CHEMBL2001
Ki 4.77 4.77 17100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 5.3 nM 8.28 Selectivity ratio of IC50 for rat P2X2 receptor to IC50 for rat P2X3 receptor 21207957
Unchecked IC50 = 6.2 nM 8.21 Selectivity ratio of IC50 for rat P2X2 receptor to IC50 for rat P2X1 receptor 21207957
Unchecked IC50 = 13.2 nM 7.88 Selectivity ratio of IC50 for rat P2X2 receptor to IC50 for rat P2X2/3 receptor 21207957
P2X purinoceptor 2 IC50 = 79.0 nM 7.1 Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte... 21207957
P2X purinoceptor 1 IC50 = 422.0 nM 6.38 Antagonist activity against rat P2X1 receptor expressed in Xenopus laevis oocyte... 21207957
P2X purinoceptor 3 IC50 = 494.0 nM 6.31 Antagonist activity against rat P2X3 receptor expressed in Xenopus laevis oocyte... 21207957
P2X purinoceptor 2 IC50 = 570.0 nM 6.24 Antagonist activity at wild type His6 tagged rat P2X1 receptor expressed in Xeno... 29649742
P2X purinoceptor 2 IC50 = 690.0 nM 6.16 Antagonist activity at human P2X2 receptor expressed in 1321N1 cells assessed as... 29649742
P2X purinoceptor 2 IC50 = 692.0 nM 6.16 Antagonist activity at human P2X2 receptor expressed in human 1321N1 cells asses... 27427902
P2X2/P2X3 receptor IC50 = 1042.0 nM 5.98 Antagonist activity against rat P2X2/3 receptor expressed in Xenopus laevis oocy... 21207957
P2X purinoceptor 1 IC50 = 4700.0 nM 5.33 Antagonist activity at P2X1 receptor in rat vas deferens assessed as inhibition ... 29649742
P2Y purinoceptor 2 IC50 = 10000.0 nM 5.0 Antagonist activity against human P2Y2 receptor expressed in 1321N1 astrocytoma ... 21207957
P2Y purinoceptor 12 Ki = 17100.0 nM 4.77 Displacement of [3H]PSB0413 from human platelet P2Y12 receptor 21207957

Literature References

PubMed DOI Target Context # Activities
21207957 10.1021/jm1012193 Unchecked 9
29649742 10.1016/j.ejmech.2018.03.023 P2X purinoceptor 2 2
29649742 10.1016/j.ejmech.2018.03.023 P2X purinoceptor 1 2
21207957 10.1021/jm1012193 P2Y purinoceptor 6 1
27427902 10.1021/acs.jmedchem.5b01690 P2X purinoceptor 4 1
27427902 10.1021/acs.jmedchem.5b01690 P2X purinoceptor 3 1
27427902 10.1021/acs.jmedchem.5b01690 P2X purinoceptor 2 1
27427902 10.1021/acs.jmedchem.5b01690 P2X purinoceptor 1 1
29649742 10.1016/j.ejmech.2018.03.023 P2X purinoceptor 4 1
29649742 10.1016/j.ejmech.2018.03.023 P2X purinoceptor 3 1
21207957 10.1021/jm1012193 P2Y purinoceptor 12 1
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2Y purinoceptor 4 1
21207957 10.1021/jm1012193 P2Y purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 7 1
21207957 10.1021/jm1012193 P2X2/P2X3 receptor 1
21207957 10.1021/jm1012193 P2X purinoceptor 3 1
21207957 10.1021/jm1012193 P2X purinoceptor 1 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1

Data from ChEMBL 36 via Core Engine