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Assay Detail

CHEMBL4430453

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Binding
Reversible inhibition of recombinant human Adk-short expressed in Escherichia coli BL21[DE3] assessed as [3H]AMP formation preincubated for 15 mins followed by [3H]adenosine addition measured after 30 mins by liquid scintillation counting method
14
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine kinase (CHEMBL3589)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Focused screening to identify new adenosine kinase inhibitors.
Köse M, Schiedel AC, Bauer AA, Poschenrieder H, Burbiel JC, Akkinepally RR, Stachel HD, Müller CE.
Bioorg Med Chem (2016) 24 : 5127 -5133
PubMed 27595538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.32 7.79
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99203 IODOTUBERCIDIN 2 7.79
CHEMBL4570031 1 6.74
CHEMBL494210 1 5.30
CHEMBL4460819 1 5.26
CHEMBL4524434 1 5.25
CHEMBL4460655 1 5.07
CHEMBL4592393 1 5.06
CHEMBL4457103 1 5.04
CHEMBL4545415 1 4.96
CHEMBL4445820 1 4.82
CHEMBL4448716 1 4.71
CHEMBL4574016 1 4.60
CHEMBL4520524 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99203 IODOTUBERCIDIN Ki = 16.3 nM 7.79
CHEMBL4570031 Ki = 184.0 nM 6.74
CHEMBL494210 Ki = 5040.0 nM 5.30
CHEMBL4460819 Ki = 5440.0 nM 5.26
CHEMBL4524434 Ki = 5640.0 nM 5.25
CHEMBL4460655 Ki = 8560.0 nM 5.07
CHEMBL4592393 Ki = 8750.0 nM 5.06
CHEMBL4457103 Ki = 9180.0 nM 5.04
CHEMBL4545415 Ki = 11100.0 nM 4.96
CHEMBL4445820 Ki = 15100.0 nM 4.82
CHEMBL4448716 Ki = 19500.0 nM 4.71
CHEMBL4574016 Ki = 25200.0 nM 4.60
CHEMBL4520524 Ki = 25400.0 nM 4.59
CHEMBL99203 IODOTUBERCIDIN Inhibition - % -