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Compound Detail

CHEMBL65665

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Nc1ncnc2nc(-c3ccc(N4CCC5(CC4)OCCO5)nc3)cc(-c3cccc(Br)c3)c12

Basic Information

ChEMBL ID CHEMBL65665
Phase Preclinical
Structure Type MOL
InChI Key HBKXXYRJGCAAMS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

519.4
MW (Da)
4.44
ALogP
8
HBA
1
HBD
99.3
PSA (Ų)
0.42
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23BrN6O2
MW 519.40
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.17

Activity Summary

IC50 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine kinase
CHEMBL3589
IC50 8.85 8.2 1.4 2

Pharmacokinetic Data

Parameter Value Units Species
F 44.7 % Rattus norvegicus
F 38.5 % Canis lupus familiaris
T1/2 2.4 hr Rattus norvegicus
T1/2 3.6 hr Rattus norvegicus
T1/2 4.1 hr Canis lupus familiaris
T1/2 3.4 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11514141 10.1016/s0960-894x(01)00375-4 Rattus norvegicus 5
11514141 10.1016/s0960-894x(01)00375-4 Canis familiaris 3
11514141 10.1016/s0960-894x(01)00375-4 Adenosine kinase 2

Data from ChEMBL 36 via Core Engine