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Compound Detail

CHEMBL5206639

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O[C@H]1CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]2[C@H]1CNCc1ccccc1

Basic Information

ChEMBL ID CHEMBL5206639
Phase Preclinical
Structure Type MOL
InChI Key ZUWKRYJSHNVYBR-ZNWNOEGYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

415.6
MW (Da)
4.26
ALogP
3
HBA
3
HBD
51.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N3O
MW 415.58
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.76

Activity Summary

IC50 1 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
IC50 6.26 6.26 545.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a IC50 = 545.7 nM 6.26 Antagonist activity at human adenosine A2A receptor 34695776

Literature References

PubMed DOI Target Context # Activities
34695776 10.1016/j.ejmech.2021.113907 Adenosine receptor A2a 2

Data from ChEMBL 36 via Core Engine