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Compound Detail

CHEMBL470942

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Nc1nc(N(CCN2CCN(c3ccc(F)cc3F)CC2)CC2CC2)cc2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL470942
Phase Preclinical
Structure Type MOL
InChI Key UUUUCFGJWJWDEN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

494.6
MW (Da)
3.28
ALogP
9
HBA
1
HBD
92.0
PSA (Ų)
0.40
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28F2N8O
MW 494.55
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -2.01

Activity Summary

Ki 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 9.52 9.52 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 17.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19109019 10.1016/j.bmcl.2008.11.075 Rattus norvegicus 5
19109019 10.1016/j.bmcl.2008.11.075 Adenosine receptor A2a 1
19109019 10.1016/j.bmcl.2008.11.075 Unchecked 1

Data from ChEMBL 36 via Core Engine