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Compound Detail

CHEMBL2111930

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[11CH3]Oc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1

Basic Information

ChEMBL ID CHEMBL2111930
Phase Preclinical
Structure Type MOL
InChI Key AEULVFLPCJOBCE-BJUDXGSMSA-N
Parent Compound CHEMBL136689
Active Moiety CHEMBL136689
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

389.4
MW (Da)
2.96
ALogP
9
HBA
1
HBD
109.3
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N7O2
MW 388.42
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.80

Activity Summary

Kd 1 meas. best 10.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL302
Kd 10.32 10.32 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Kd = 0.048 nM 10.32 Binding affinity to adenosine receptor A2a in rat striatum 24164628

Literature References

PubMed DOI Target Context # Activities
11087559 10.1021/jm0009843 Rattus norvegicus 105
24164628 10.1021/jm4011669 Adenosine receptor A2a 1

Data from ChEMBL 36 via Core Engine