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Assay Detail

CHEMBL643555

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Binding
Inhibition adenosine kinase activity in rat brain in vitro
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine kinase (CHEMBL2384)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.
Perner RJ, Gu YG, Lee CH, Bayburt EK, McKie J, Alexander KM, Kohlhaas KL, Wismer CT, Mikusa J, Jarvis MF, Kowaluk EA, Bhagwat SS.
J Med Chem (2003) 46 : 5249 -5257
PubMed 14613327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.79 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150370 1 9.60
CHEMBL150478 1 9.37
CHEMBL348712 1 9.26
CHEMBL356896 1 9.01
CHEMBL346622 1 8.52
CHEMBL342310 1 8.51
CHEMBL151448 1 8.49
CHEMBL151812 1 8.40
CHEMBL151214 1 8.30
CHEMBL422489 1 8.30
CHEMBL151079 1 8.17
CHEMBL68492 1 8.15
CHEMBL356256 1 7.80
CHEMBL358714 1 7.43
CHEMBL435646 1 7.26
CHEMBL265251 1 7.22
CHEMBL439635 1 7.20
CHEMBL147390 1 6.52
CHEMBL150978 1 6.46
CHEMBL147356 1 6.40
CHEMBL151553 1 6.39
CHEMBL66338 1 6.36
CHEMBL303499 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150370 IC50 = 0.25 nM 9.60
CHEMBL150478 IC50 = 0.43 nM 9.37
CHEMBL348712 IC50 = 0.55 nM 9.26
CHEMBL356896 IC50 = 0.98 nM 9.01
CHEMBL346622 IC50 = 3.0 nM 8.52
CHEMBL342310 IC50 = 3.1 nM 8.51
CHEMBL151448 IC50 = 3.2 nM 8.49
CHEMBL151812 IC50 = 4.0 nM 8.40
CHEMBL151214 IC50 = 5.0 nM 8.30
CHEMBL422489 IC50 = 5.0 nM 8.30
CHEMBL151079 IC50 = 6.7 nM 8.17
CHEMBL68492 IC50 = 7.0 nM 8.15
CHEMBL356256 IC50 = 16.0 nM 7.80
CHEMBL358714 IC50 = 37.0 nM 7.43
CHEMBL435646 IC50 = 55.0 nM 7.26
CHEMBL265251 IC50 = 60.0 nM 7.22
CHEMBL439635 IC50 = 63.0 nM 7.20
CHEMBL147390 IC50 = 300.0 nM 6.52
CHEMBL150978 IC50 = 350.0 nM 6.46
CHEMBL147356 IC50 = 400.0 nM 6.40
CHEMBL151553 IC50 = 410.0 nM 6.39
CHEMBL66338 IC50 = 440.0 nM 6.36
CHEMBL303499 IC50 = 773.0 nM 6.11