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Compound Detail

CHEMBL208920

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CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC(C)C)c1=O

Basic Information

ChEMBL ID CHEMBL208920
Phase Preclinical
Structure Type MOL
InChI Key PTIXDWKOEDXQSV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
4.13
ALogP
7
HBA
1
HBD
90.5
PSA (Ų)
0.42
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27F3N6O2
MW 488.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.56

Activity Summary

Ki 3 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2b
CHEMBL255
Ki 6.52 6.52 300.0 1
Adenosine receptor A1
CHEMBL226
Ki 5.51 5.51 3100.0 1
Adenosine receptor A2a
CHEMBL251
Ki 5.37 5.37 4300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16759111 10.1021/jm051268+ Adenosine receptor A2b 1
16759111 10.1021/jm051268+ Adenosine receptor A1 1
16759111 10.1021/jm051268+ Adenosine receptor A2a 1
16759111 10.1021/jm051268+ Adenosine receptors; A1 & A2b 1
16759111 10.1021/jm051268+ Adenosine A2 receptor 1

Data from ChEMBL 36 via Core Engine