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Compound Detail

CHEMBL1775009

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Nc1ncnc2c1nc(Br)n2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL1775009
Phase Preclinical
Structure Type MOL
InChI Key VJUPMOPLUQHMLE-UUOKFMHZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

346.1
MW (Da)
-1.22
ALogP
9
HBA
4
HBD
139.5
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C10H12BrN5O4
MW 346.14
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness 0.86

Activity Summary

Ki 1 meas. best 4.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL302
Ki 4.64 4.64 22700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2a Ki = 22700.0 nM 4.64 Binding affinity to adenosine A2A receptor in rat striatal membranes by measurin... 7707320

Literature References

PubMed DOI Target Context # Activities
3862866 10.1021/jm00148a018 Erythroleukemia cell line 6
966249 10.1021/jm00230a011 Unchecked 2
6279840 10.1021/jm00345a001 Adenosine receptor A1 1
6279840 10.1021/jm00345a001 Adenosine A2 receptor 1
6279840 10.1021/jm00345a001 Adenosine receptor 1
7707320 10.1021/jm00007a014 Adenosine receptor A1 1
7707320 10.1021/jm00007a014 Adenosine receptor A2a 1
7707320 10.1021/jm00007a014 Adenosine receptor A3 1
21528845 10.1021/jm1013852 NAD-dependent protein deacetylase sirtuin-1 1
21528845 10.1021/jm1013852 NAD-dependent protein deacetylase sirtuin-2 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1

Data from ChEMBL 36 via Core Engine