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Compound Detail

CHEMBL439868

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CC(=O)c1ccc(NC(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cc1

Basic Information

ChEMBL ID CHEMBL439868
Phase Preclinical
Structure Type MOL
InChI Key XGWSSATXJAYXNU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
2.45
ALogP
7
HBA
2
HBD
115.2
PSA (Ų)
0.44
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 C24H22N4O5
MW 446.46
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.18

Activity Summary

Ki 1 meas. best 8.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2b
CHEMBL255
Ki 8.45 8.45 3.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2b Ki = 3.548 nM 8.45 Binding affinity to recombinant human adenosine A2B receptor 16392813

Literature References

PubMed DOI Target Context # Activities
16392813 10.1021/jm0506221 Adenosine receptor A2b 3
16392813 10.1021/jm0506221 Adenosine receptor A2a 1

Data from ChEMBL 36 via Core Engine