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Assay Detail

CHEMBL829686

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

Binding
Inhibition constant against human Adenosine A2a receptor using [3H]-SCH- 58261 as radioligand expressed in HEK cell membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Kiselgof E, Tulshian DB, Arik L, Zhang H, Fawzi A.
Bioorg Med Chem Lett (2005) 15 : 2119 -2122
PubMed 15808481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.89 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195364 1 8.85
CHEMBL372475 1 8.55
CHEMBL195503 1 8.51
CHEMBL17127 SCH-58261 1 8.37
CHEMBL371615 1 8.35
CHEMBL193613 1 8.25
CHEMBL195543 1 8.20
CHEMBL193761 1 8.17
CHEMBL193414 1 8.15
CHEMBL195410 1 8.11
CHEMBL197148 1 8.06
CHEMBL195294 1 8.00
CHEMBL371436 1 7.91
CHEMBL424827 1 7.69
CHEMBL195330 1 7.67
CHEMBL195866 1 7.66
CHEMBL372928 1 7.58
CHEMBL196436 1 7.46
CHEMBL439336 1 7.16
CHEMBL194383 1 6.57
CHEMBL372064 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195364 Ki = 1.4 nM 8.85
CHEMBL372475 Ki = 2.8 nM 8.55
CHEMBL195503 Ki = 3.1 nM 8.51
CHEMBL17127 SCH-58261 Ki = 4.3 nM 8.37
CHEMBL371615 Ki = 4.5 nM 8.35
CHEMBL193613 Ki = 5.6 nM 8.25
CHEMBL195543 Ki = 6.3 nM 8.20
CHEMBL193761 Ki = 6.8 nM 8.17
CHEMBL193414 Ki = 7.1 nM 8.15
CHEMBL195410 Ki = 7.7 nM 8.11
CHEMBL197148 Ki = 8.7 nM 8.06
CHEMBL195294 Ki = 10.0 nM 8.00
CHEMBL371436 Ki = 12.3 nM 7.91
CHEMBL424827 Ki = 20.5 nM 7.69
CHEMBL195330 Ki = 21.5 nM 7.67
CHEMBL195866 Ki = 22.0 nM 7.66
CHEMBL372928 Ki = 26.0 nM 7.58
CHEMBL196436 Ki = 34.9 nM 7.46
CHEMBL439336 Ki = 68.5 nM 7.16
CHEMBL194383 Ki = 270.5 nM 6.57
CHEMBL372064 Ki = 381.0 nM 6.42