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Assay Detail

CHEMBL872316

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory concentration against human recombinant adenosine kinase using [14C]AMP as radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine kinase (CHEMBL3589)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adenosine kinase inhibitors. 5. Synthesis, enzyme inhibition, and analgesic activity of diaryl-erythro-furanosyltubercidin analogues.
Boyer SH, Ugarkar BG, Solbach J, Kopcho J, Matelich MC, Ollis K, Gomez-Galeno JE, Mendonca R, Tsuchiya M, Nagahisa A, Nakane M, Wiesner JB, Erion MD.
J Med Chem (2005) 48 : 6430 -6441
PubMed 16190769 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.18 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194294 1 9.52
CHEMBL343247 1 9.33
CHEMBL100421 1 9.30
CHEMBL319315 1 9.10
CHEMBL436598 1 9.10
CHEMBL370218 1 9.00
CHEMBL435120 1 8.70
CHEMBL371704 1 8.70
CHEMBL197756 1 8.52
CHEMBL364049 1 8.40
CHEMBL373218 1 8.40
CHEMBL381682 1 8.30
CHEMBL196483 1 8.28
CHEMBL194952 1 8.22
CHEMBL197801 1 8.22
CHEMBL198143 1 8.15
CHEMBL66280 5-IODO,5'-DEOXYTUBERCIDIN 1 8.05
CHEMBL380998 1 8.00
CHEMBL99203 IODOTUBERCIDIN 1 7.58
CHEMBL356952 1 7.17
CHEMBL145388 1 6.40
CHEMBL373104 1 6.22
CHEMBL364265 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194294 IC50 = 0.3 nM 9.52
CHEMBL343247 IC50 = 0.47 nM 9.33
CHEMBL100421 IC50 = 0.5 nM 9.30
CHEMBL319315 IC50 = 0.8 nM 9.10
CHEMBL436598 IC50 = 0.8 nM 9.10
CHEMBL370218 IC50 = 1.0 nM 9.00
CHEMBL435120 IC50 = 2.0 nM 8.70
CHEMBL371704 IC50 = 2.0 nM 8.70
CHEMBL197756 IC50 = 3.0 nM 8.52
CHEMBL364049 IC50 = 4.0 nM 8.40
CHEMBL373218 IC50 = 4.0 nM 8.40
CHEMBL381682 IC50 = 5.0 nM 8.30
CHEMBL196483 IC50 = 5.3 nM 8.28
CHEMBL194952 IC50 = 6.0 nM 8.22
CHEMBL197801 IC50 = 6.0 nM 8.22
CHEMBL198143 IC50 = 7.0 nM 8.15
CHEMBL66280 5-IODO,5'-DEOXYTUBERCIDIN IC50 = 9.0 nM 8.05
CHEMBL380998 IC50 = 10.0 nM 8.00
CHEMBL99203 IODOTUBERCIDIN IC50 = 26.0 nM 7.58
CHEMBL356952 IC50 = 68.0 nM 7.17
CHEMBL145388 IC50 = 400.0 nM 6.40
CHEMBL373104 IC50 = 600.0 nM 6.22
CHEMBL364265 IC50 = 4000.0 nM 5.40