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Assay Detail

CHEMBL917987

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

Binding
Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
Volpini R, Dal Ben D, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G.
J Med Chem (2007) 50 : 1222 -1230
PubMed 17309246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 5.35 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223326 1 7.04
CHEMBL220889 1 6.57
CHEMBL375190 1 6.44
CHEMBL223270 1 6.21
CHEMBL219888 1 6.12
CHEMBL220158 1 5.75
CHEMBL1162942 1 5.75
CHEMBL375619 1 5.74
CHEMBL385770 1 5.57
CHEMBL223327 1 5.53
CHEMBL220335 1 5.51
CHEMBL223740 1 5.50
CHEMBL374019 1 5.50
CHEMBL223739 1 5.40
CHEMBL223786 1 5.38
CHEMBL441707 1 5.37
CHEMBL374792 1 5.34
CHEMBL375301 1 5.28
CHEMBL267421 1 5.24
CHEMBL220386 1 5.20
CHEMBL220899 1 5.20
CHEMBL374462 1 5.19
CHEMBL374320 1 5.19
CHEMBL374242 1 5.18
CHEMBL373578 1 5.08
CHEMBL223625 1 4.98
CHEMBL385771 1 4.92
CHEMBL223472 1 4.91
CHEMBL223328 1 4.90
CHEMBL223456 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223326 Ki = 91.0 nM 7.04
CHEMBL220889 Ki = 267.0 nM 6.57
CHEMBL375190 Ki = 363.0 nM 6.44
CHEMBL223270 Ki = 620.0 nM 6.21
CHEMBL219888 Ki = 758.0 nM 6.12
CHEMBL220158 Ki = 1780.0 nM 5.75
CHEMBL1162942 Ki = 1760.0 nM 5.75
CHEMBL375619 Ki = 1820.0 nM 5.74
CHEMBL385770 Ki = 2680.0 nM 5.57
CHEMBL223327 Ki = 2960.0 nM 5.53
CHEMBL220335 Ki = 3080.0 nM 5.51
CHEMBL223740 Ki = 3130.0 nM 5.50
CHEMBL374019 Ki = 3140.0 nM 5.50
CHEMBL223739 Ki = 3960.0 nM 5.40
CHEMBL223786 Ki = 4210.0 nM 5.38
CHEMBL441707 Ki = 4290.0 nM 5.37
CHEMBL374792 Ki = 4600.0 nM 5.34
CHEMBL375301 Ki = 5290.0 nM 5.28
CHEMBL267421 Ki = 5740.0 nM 5.24
CHEMBL220899 Ki = 6310.0 nM 5.20
CHEMBL220386 Ki = 6290.0 nM 5.20
CHEMBL374462 Ki = 6460.0 nM 5.19
CHEMBL374320 Ki = 6520.0 nM 5.19
CHEMBL374242 Ki = 6660.0 nM 5.18
CHEMBL373578 Ki = 8270.0 nM 5.08
CHEMBL223625 Ki = 10400.0 nM 4.98
CHEMBL385771 Ki = 12100.0 nM 4.92
CHEMBL223472 Ki = 12400.0 nM 4.91
CHEMBL223328 Ki = 12500.0 nM 4.90
CHEMBL223456 Ki = 14700.0 nM 4.83
CHEMBL221206 Ki = 16300.0 nM 4.79
CHEMBL223514 Ki = 18000.0 nM 4.75
CHEMBL427077 Ki = 18700.0 nM 4.73
CHEMBL374336 Ki = 27100.0 nM 4.57
CHEMBL220334 Ki = 31700.0 nM 4.50
CHEMBL426537 Ki = 35100.0 nM 4.46