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Compound Detail

CHEMBL480397

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Nc1nc(OCCN2CCN(c3ccc(F)cc3F)CC2)cc2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL480397
Phase Preclinical
Structure Type MOL
InChI Key PCMOYYLIFWTHMQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

441.4
MW (Da)
2.45
ALogP
9
HBA
1
HBD
98.0
PSA (Ų)
0.49
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 C21H21F2N7O2
MW 441.44
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -2.19

Activity Summary

Ki 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 187.0 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 4
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