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Compound Detail

CHEMBL469877

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Nc1nc2c(cnn2CCN2CCc3ccccc3C2)c2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL469877
Phase Preclinical
Structure Type MOL
InChI Key OTQDGXDYTSLVAQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
2.37
ALogP
9
HBA
1
HBD
103.3
PSA (Ų)
0.49
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 C21H20N8O
MW 400.45
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.99

Activity Summary

Ki 1 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 8.39 8.39 4.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 60.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 4.1 nM 8.39 Antagonist activity at human adenosine A2A receptor 18558486

Literature References

PubMed DOI Target Context # Activities
18558486 10.1016/j.bmcl.2008.05.069 Rattus norvegicus 3
18558486 10.1016/j.bmcl.2008.05.069 Adenosine receptor A2a 1
18558486 10.1016/j.bmcl.2008.05.069 Unchecked 1
18558486 10.1016/j.bmcl.2008.05.069 No relevant target 1

Data from ChEMBL 36 via Core Engine