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Compound Detail

CHEMBL413145

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O=C(Nc1cccc(C(=O)Nc2cc(C(=O)Nc3ccc(S(=O)(=O)[O-])c4cc(S(=O)(=O)[O-])cc(S(=O)(=O)[O-])c34)ccc2F)c1)Nc1cccc(C(=O)Nc2cc(C(=O)Nc3ccc(S(=O)(=O)[O-])c4cc(S(=O)(=O)[O-])cc(S(=O)(=O)[O-])c34)ccc2F)c1.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL413145
Phase Preclinical
Structure Type MOL
InChI Key PFKJKZYADCSCBI-UHFFFAOYSA-H
Parent Compound CHEMBL1207514
Active Moiety CHEMBL1207514
7
Targets
10
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

1305.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C49H28F2N6Na6O23S6
MW 1437.12

Activity Summary

IC50 9 meas. best 7.38
Ki 1 meas. best 7.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.38 7.38 42.0 1
P2Y purinoceptor 11
CHEMBL4867
Ki 7.35 7.35 44.7 1
P2X purinoceptor 1
CHEMBL2094
IC50 7.2 7.2 63.1 1
P2X purinoceptor 4
CHEMBL2818
IC50 7.09 7.09 81.3 1
P2X purinoceptor 2
CHEMBL2135
IC50 6.86 6.86 138.0 1
P2X purinoceptor 3
CHEMBL2998
IC50 6.45 6.45 354.8 1
P2Y purinoceptor 11
CHEMBL4867
IC50 6.34 6.34 457.1 1
P2X purinoceptor 3
CHEMBL4824
IC50 6.11 6.11 776.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16250663 10.1021/jm050301p P2Y purinoceptor 11 4
16250663 10.1021/jm050301p P2X purinoceptor 4 3
16250663 10.1021/jm050301p P2Y purinoceptor 1 2
16250663 10.1021/jm050301p P2X purinoceptor 3 2
16250663 10.1021/jm050301p P2Y purinoceptor 2 2
16250663 10.1021/jm050301p P2X purinoceptor 7 1
16250663 10.1021/jm050301p P2X purinoceptor 1 1
16250663 10.1021/jm050301p P2X purinoceptor 2 1
23680445 10.1016/j.bmc.2013.04.047 Unchecked 1

Data from ChEMBL 36 via Core Engine