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Compound Detail

CHEMBL472111

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Nc1nc2c(cnn2CCN2CCc3ccc([N+](=O)[O-])cc3CC2)c2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL472111
Phase Preclinical
Structure Type MOL
InChI Key FWZQSNQBDAECAU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
2.33
ALogP
11
HBA
1
HBD
146.4
PSA (Ų)
0.31
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N9O3
MW 459.47
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -2.05

Activity Summary

Ki 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 9.15 9.15 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 0.7 nM 9.15 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