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Compound Detail

CHEMBL446621

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Cc1nn(C)c(Cl)c1CNC[C@H]1CC[C@H]2CN(c3nc(N)n4nc(-c5ccco5)nc4n3)CCN2C1

Basic Information

ChEMBL ID CHEMBL446621
Phase Preclinical
Structure Type MOL
InChI Key VLARWIPUMWYZST-CVEARBPZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

512.0
MW (Da)
1.75
ALogP
12
HBA
2
HBD
131.5
PSA (Ų)
0.39
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30ClN11O
MW 512.02
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -2.04

Activity Summary

Ki 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL302
Ki 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 30.0 nM 7.52 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