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Assay Detail

CHEMBL645535

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Binding
In vitro concentration required for 50% inhibition against Adenosine Kinase (AK) in the presence of intact cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Adenosine kinase (CHEMBL3589)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyridopyrimidine analogues as novel adenosine kinase inhibitors.
Zheng GZ, Lee C, Pratt JK, Perner RJ, Jiang MQ, Gomtsyan A, Matulenko MA, Mao Y, Koenig JR, Kim KH, Muchmore S, Yu H, Kohlhaas K, Alexander KM, McGaraughty S, Chu KL, Wismer CT, Mikusa J, Jarvis MF, Marsh K, Kowaluk EA, Bhagwat SS, Stewart AO.
Bioorg Med Chem Lett (2001) 11 : 2071 -2074
PubMed 11514141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.38 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65665 1 7.55
CHEMBL62974 1 7.48
CHEMBL62342 1 7.42
CHEMBL62524 1 7.37
CHEMBL62576 1 7.37
CHEMBL66089 1 7.36
CHEMBL302404 1 7.35
CHEMBL65664 1 7.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65665 IC50 = 28.3 nM 7.55
CHEMBL62974 IC50 = 33.0 nM 7.48
CHEMBL62342 IC50 = 37.7 nM 7.42
CHEMBL62524 IC50 = 42.3 nM 7.37
CHEMBL62576 IC50 = 42.5 nM 7.37
CHEMBL66089 IC50 = 43.3 nM 7.36
CHEMBL302404 IC50 = 45.0 nM 7.35
CHEMBL65664 IC50 = 70.9 nM 7.15