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Compound Detail

CHEMBL4755127

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CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL4755127
Phase Preclinical
Structure Type MOL
InChI Key WZEOUDCZNWYPNQ-BNVVKXJLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
-0.29
ALogP
10
HBA
5
HBD
154.7
PSA (Ų)
0.33
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N6O5
MW 452.47
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness 0.32

Activity Summary

Ki 1 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A3
CHEMBL256
Ki 9.12 9.12 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A3 Ki = 0.75 nM 9.12 Binding affinity to human A3AR assessed as inhibitor constant 33062176

Literature References

PubMed DOI Target Context # Activities
33062176 10.1021/acsmedchemlett.9b00637 Adenosine receptor A3 1

Data from ChEMBL 36 via Core Engine