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Compound Detail

CHEMBL246468

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COCCOc1ccc(N2CCN(CCn3cnc4c3nc(N)n3nc(-c5ccccc5)nc43)CC2)cc1

Basic Information

ChEMBL ID CHEMBL246468
Phase Preclinical
Structure Type MOL
InChI Key UMITUBMNAWNEIW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

513.6
MW (Da)
2.57
ALogP
11
HBA
1
HBD
111.9
PSA (Ų)
0.30
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N9O2
MW 513.61
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.55

Activity Summary

Ki 1 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 8.43 8.43 3.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 3.7 nM 8.43 Antagonist activity at human adenosine A2A receptor 17234414

Literature References

PubMed DOI Target Context # Activities
17234414 10.1016/j.bmcl.2006.12.104 Adenosine receptor A2a 1
17234414 10.1016/j.bmcl.2006.12.104 Unchecked 1

Data from ChEMBL 36 via Core Engine