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Assay Detail

CHEMBL649880

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

Binding
Binding affinity against Adenosine-2 receptor with [3H]-NECA in rat striatal membranes.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.
Trivedi BK, Bruns RF.
J Med Chem (1988) 31 : 1011 -1014
PubMed 3361571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.33 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268071 1 6.00
CHEMBL414401 1 5.77
CHEMBL266978 1 5.74
CHEMBL267400 1 5.57
CHEMBL7271 1 5.52
CHEMBL7472 1 5.40
CHEMBL6958 1 5.38
CHEMBL6890 1 5.35
CHEMBL268801 1 5.21
CHEMBL269044 1 5.17
CHEMBL269318 1 5.16
CHEMBL7325 1 4.93
CHEMBL7033 1 4.73
CHEMBL7219 1 4.66
CHEMBL7454 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268071 Ki = 1010.0 nM 6.00
CHEMBL414401 Ki = 1710.0 nM 5.77
CHEMBL266978 Ki = 1830.0 nM 5.74
CHEMBL267400 Ki = 2700.0 nM 5.57
CHEMBL7271 Ki = 3000.0 nM 5.52
CHEMBL7472 Ki = 4000.0 nM 5.40
CHEMBL6958 Ki = 4200.0 nM 5.38
CHEMBL6890 Ki = 4500.0 nM 5.35
CHEMBL268801 Ki = 6100.0 nM 5.21
CHEMBL269044 Ki = 6700.0 nM 5.17
CHEMBL269318 Ki = 7000.0 nM 5.16
CHEMBL7325 Ki = 11800.0 nM 4.93
CHEMBL7033 Ki = 18800.0 nM 4.73
CHEMBL7219 Ki = 22000.0 nM 4.66
CHEMBL7454 Ki > 10000.0 nM -