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Assay Detail

CHEMBL643554

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

Binding
In vitro inhibition of Adenosine kinase of rat brain cytosol.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine kinase (CHEMBL2384)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors.
Lee CH, Daanen JF, Jiang M, Yu H, Kohlhaas KL, Alexander K, Jarvis MF, Kowaluk EL, Bhagwat SS.
Bioorg Med Chem Lett (2001) 11 : 2419 -2422
PubMed 11549437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.74 8.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66280 5-IODO,5'-DEOXYTUBERCIDIN 1 8.79
CHEMBL81198 1 8.70
CHEMBL407574 1 8.40
CHEMBL302376 1 7.82
CHEMBL312260 1 7.46
CHEMBL80588 1 6.22
CHEMBL304179 1 5.70
CHEMBL81063 1 5.40
CHEMBL81628 1 5.40
CHEMBL311217 1 5.21
CHEMBL77678 1 5.00
CHEMBL310806 1 -
CHEMBL311898 1 -
CHEMBL78716 1 -
CHEMBL81054 1 -
CHEMBL309926 1 -
CHEMBL312683 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66280 5-IODO,5'-DEOXYTUBERCIDIN IC50 = 1.63 nM 8.79
CHEMBL81198 IC50 = 2.0 nM 8.70
CHEMBL407574 IC50 = 4.0 nM 8.40
CHEMBL302376 IC50 = 15.0 nM 7.82
CHEMBL312260 IC50 = 35.0 nM 7.46
CHEMBL80588 IC50 = 600.0 nM 6.22
CHEMBL304179 IC50 = 2000.0 nM 5.70
CHEMBL81063 IC50 = 4000.0 nM 5.40
CHEMBL81628 IC50 = 4000.0 nM 5.40
CHEMBL311217 IC50 = 6100.0 nM 5.21
CHEMBL77678 IC50 = 10000.0 nM 5.00
CHEMBL310806 IC50 > 10000.0 nM -
CHEMBL311898 IC50 > 10000.0 nM -
CHEMBL78716 IC50 > 10000.0 nM -
CHEMBL81054 IC50 > 10000.0 nM -
CHEMBL309926 IC50 > 10000.0 nM -
CHEMBL312683 IC50 > 10000.0 nM -