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Assay Detail

CHEMBL642180

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Binding
Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
Vittori S, Lorenzen A, Stannek C, Costanzi S, Volpini R, IJzerman AP, Kunzel JK, Cristalli G.
J Med Chem (2000) 43 : 250 -260
PubMed 10649980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 5.52 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569275 1 6.38
CHEMBL2113520 1 6.34
CHEMBL2113423 1 6.29
CHEMBL2113517 1 6.23
CHEMBL45891 1 6.22
CHEMBL284969 1 6.19
CHEMBL608306 1 5.96
CHEMBL2113518 1 5.69
CHEMBL2113390 1 5.55
CHEMBL2113477 1 5.51
CHEMBL2113430 1 5.50
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 5.47
CHEMBL2113424 1 5.38
CHEMBL607729 1 5.37
CHEMBL312981 1 5.31
CHEMBL2113387 1 5.29
CHEMBL2113391 1 5.28
CHEMBL2113516 1 5.18
CHEMBL611851 1 5.04
CHEMBL2113521 1 5.02
CHEMBL2113389 1 5.00
CHEMBL606228 1 4.86
CHEMBL2113478 1 4.79
CHEMBL604965 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569275 Ki = 420.0 nM 6.38
CHEMBL2113520 Ki = 460.0 nM 6.34
CHEMBL2113423 Ki = 510.0 nM 6.29
CHEMBL2113517 Ki = 590.0 nM 6.23
CHEMBL45891 Ki = 600.0 nM 6.22
CHEMBL284969 Ki = 640.0 nM 6.19
CHEMBL608306 Ki = 1100.0 nM 5.96
CHEMBL2113518 Ki = 2060.0 nM 5.69
CHEMBL2113390 Ki = 2840.0 nM 5.55
CHEMBL2113477 Ki = 3110.0 nM 5.51
CHEMBL2113430 Ki = 3150.0 nM 5.50
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 3370.0 nM 5.47
CHEMBL2113424 Ki = 4180.0 nM 5.38
CHEMBL607729 Ki = 4230.0 nM 5.37
CHEMBL312981 Ki = 4870.0 nM 5.31
CHEMBL2113387 Ki = 5120.0 nM 5.29
CHEMBL2113391 Ki = 5210.0 nM 5.28
CHEMBL2113516 Ki = 6550.0 nM 5.18
CHEMBL611851 Ki = 9200.0 nM 5.04
CHEMBL2113521 Ki = 9640.0 nM 5.02
CHEMBL2113389 Ki = 10100.0 nM 5.00
CHEMBL606228 Ki = 13700.0 nM 4.86
CHEMBL2113478 Ki = 16400.0 nM 4.79
CHEMBL604965 Ki = 20000.0 nM 4.70