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Assay Detail

CHEMBL644389

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

Binding
Binding affinity towards human adenosine A3 receptor expressed in HEK293 cells in presence of [125I]-AB-MECA at a concentration of 1 uM
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.
Colotta V, Catarzi D, Varano F, Cecchi L, Filacchioni G, Martini C, Trincavelli L, Lucacchini A.
J Med Chem (2000) 43 : 1158 -1164
PubMed 10737748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.08 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16488 1 8.83
CHEMBL16305 1 8.70
CHEMBL280080 1 8.43
CHEMBL16737 1 7.80
CHEMBL274273 1 7.80
CHEMBL279410 1 7.60
CHEMBL276321 1 7.56
CHEMBL416537 1 7.54
CHEMBL16510 1 7.44
CHEMBL16195 1 7.39
CHEMBL279870 1 7.36
CHEMBL16416 1 7.34
CHEMBL273578 1 7.32
CHEMBL280278 1 7.26
CHEMBL16715 1 7.25
CHEMBL16750 1 7.20
CHEMBL16242 1 7.10
CHEMBL280300 1 7.04
CHEMBL276528 1 6.94
CHEMBL276545 1 6.86
CHEMBL16643 1 6.80
CHEMBL16774 1 6.76
CHEMBL16539 1 6.71
CHEMBL16529 1 6.70
CHEMBL16254 1 6.56
CHEMBL16820 1 6.48
CHEMBL16833 1 6.32
CHEMBL274267 1 6.30
CHEMBL422750 1 6.30
CHEMBL275421 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16488 Ki = 1.47 nM 8.83
CHEMBL16305 Ki = 2.0 nM 8.70
CHEMBL280080 Ki = 3.75 nM 8.43
CHEMBL16737 Ki = 16.0 nM 7.80
CHEMBL274273 Ki = 15.8 nM 7.80
CHEMBL279410 Ki = 25.0 nM 7.60
CHEMBL276321 Ki = 27.5 nM 7.56
CHEMBL416537 Ki = 28.5 nM 7.54
CHEMBL16510 Ki = 36.6 nM 7.44
CHEMBL16195 Ki = 40.9 nM 7.39
CHEMBL279870 Ki = 44.2 nM 7.36
CHEMBL16416 Ki = 45.3 nM 7.34
CHEMBL273578 Ki = 48.3 nM 7.32
CHEMBL280278 Ki = 55.4 nM 7.26
CHEMBL16715 Ki = 56.1 nM 7.25
CHEMBL16750 Ki = 63.0 nM 7.20
CHEMBL16242 Ki = 80.0 nM 7.10
CHEMBL280300 Ki = 91.0 nM 7.04
CHEMBL276528 Ki = 114.0 nM 6.94
CHEMBL276545 Ki = 137.0 nM 6.86
CHEMBL16643 Ki = 157.0 nM 6.80
CHEMBL16774 Ki = 173.0 nM 6.76
CHEMBL16539 Ki = 197.0 nM 6.71
CHEMBL16529 Ki = 201.0 nM 6.70
CHEMBL16254 Ki = 276.0 nM 6.56
CHEMBL16820 Ki = 329.0 nM 6.48
CHEMBL16833 Ki = 479.0 nM 6.32
CHEMBL274267 Ki = 506.0 nM 6.30
CHEMBL422750 Ki = 504.0 nM 6.30
CHEMBL275421 Ki = 548.0 nM 6.26
CHEMBL16215 Ki = 960.0 nM 6.02
CHEMBL277357 Ki = 1246.0 nM 5.90
CHEMBL16598 Ki = 1700.0 nM 5.77