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Compound Detail

CHEMBL401735

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COc1ccc(Nc2cc(S(=O)(=O)[O-])c(N)c3c2C(=O)c2ccccc2C3=O)cc1.[Na+]

Basic Information

ChEMBL ID CHEMBL401735
Phase Preclinical
Structure Type MOL
InChI Key UKZVMBMYDRZSBX-UHFFFAOYSA-M
Parent Compound CHEMBL1207381
Active Moiety CHEMBL1207381
4
Targets
13
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

424.4
MW (Da)
3.04
ALogP
7
HBA
3
HBD
135.8
PSA (Ų)
0.34
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H15N2NaO6S
MW 446.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.30

Activity Summary

IC50 12 meas. best 5.76
EC50 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 2
CHEMBL4398
EC50 7.09 7.09 80.4 1
P2X purinoceptor 2
CHEMBL2135
IC50 5.76 5.76 1730.0 1
P2Y purinoceptor 4
CHEMBL2123
IC50 5.59 5.59 2590.0 1
P2Y purinoceptor 2
CHEMBL4398
IC50 5.46 4.7767 3440.0 9
P2Y purinoceptor 2
CHEMBL1075298
IC50 4.77 4.77 17000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 2 EC50 = 80.4 nM 7.09 Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor... 19419204
P2X purinoceptor 2 IC50 = 1730.0 nM 5.76 Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte... 21207957
P2Y purinoceptor 4 IC50 = 2590.0 nM 5.59 Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells ass... 28306255
P2Y purinoceptor 2 IC50 = 3440.0 nM 5.46 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mu... 19419204
P2Y purinoceptor 2 IC50 = 11500.0 nM 4.94 Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed ... 18006312
P2Y purinoceptor 2 IC50 = 17000.0 nM 4.77 Antagonist activity at mouse P2Y2 receptor in mouse NG108-15 cells assessed as i... 18006312
P2Y purinoceptor 2 IC50 = 17600.0 nM 4.75 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194A mu... 19419204
P2Y purinoceptor 2 IC50 = 21100.0 nM 4.68 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mu... 19419204
P2Y purinoceptor 2 IC50 = 21900.0 nM 4.66 Antagonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 recep... 19419204
P2Y purinoceptor 2 IC50 = 21700.0 nM 4.66 Antagonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 recep... 19419204
P2Y purinoceptor 2 IC50 = 22400.0 nM 4.65 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mu... 19419204
P2Y purinoceptor 2 IC50 = 24600.0 nM 4.61 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mu... 19419204
P2Y purinoceptor 2 IC50 = 26500.0 nM 4.58 Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R1... 19419204

Literature References

PubMed DOI Target Context # Activities
19419204 10.1021/jm801442p P2Y purinoceptor 2 14
18006312 10.1016/j.bmcl.2007.10.082 P2Y purinoceptor 2 2
21207957 10.1021/jm1012193 P2X purinoceptor 2 1
21207957 10.1021/jm1012193 P2X purinoceptor 4 1
28306255 10.1021/acs.jmedchem.7b00030 P2Y purinoceptor 4 1

Data from ChEMBL 36 via Core Engine