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Compound Detail

CHEMBL387318

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Nc1nc(N2CCN3C[C@H](COc4ccccn4)CC[C@H]3C2)nc2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL387318
Phase Preclinical
Structure Type MOL
InChI Key XSSSZWNOKWNALH-CVEARBPZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
1.74
ALogP
11
HBA
1
HBD
123.7
PSA (Ų)
0.48
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 C22H25N9O2
MW 447.50
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -2.01

Activity Summary

Ki 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL302
Ki 7.39 7.39 41.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 41.0 nM 7.39 Displacement of [3H]ZM241385 from adenosine A2A receptor in rat brain membrane 15566292

Literature References

PubMed DOI Target Context # Activities
15566292 10.1021/jm0494321 Adenosine receptor A2a 1
15566292 10.1021/jm0494321 Adenosine receptor A1 1

Data from ChEMBL 36 via Core Engine