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Assay Detail

CHEMBL646602

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

Binding
Ability to displace radioligand [125I]AB-MECA from membrane of HEK 293 cells stably transfected with human adenosine A3 receptor cDNA
13
Total Activities
13
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

5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
de Zwart M, Kourounakis A, Kooijman H, Spek AL, Link R, von Frijtag Drabbe Künzel JK, IJzerman AP.
J Med Chem (1999) 42 : 1384 -1392
PubMed 10212124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.84 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519809 1 8.19
CHEMBL464859 NECA 1 7.97
CHEMBL2070507 1 7.64
CHEMBL2070508 1 7.50
CHEMBL1235128 1 7.36
CHEMBL2113434 1 7.07
CHEMBL261482 1 6.97
CHEMBL606095 1 6.68
CHEMBL2070399 1 6.49
CHEMBL2113431 1 6.25
CHEMBL2113435 1 6.14
CHEMBL2113421 1 5.64
CHEMBL2113436 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519809 Ki = 6.4 nM 8.19
CHEMBL464859 NECA Ki = 10.6 nM 7.97
CHEMBL2070507 Ki = 23.0 nM 7.64
CHEMBL2070508 Ki = 32.0 nM 7.50
CHEMBL1235128 Ki = 44.0 nM 7.36
CHEMBL2113434 Ki = 85.3 nM 7.07
CHEMBL261482 Ki = 108.0 nM 6.97
CHEMBL606095 Ki = 211.0 nM 6.68
CHEMBL2070399 Ki = 322.0 nM 6.49
CHEMBL2113431 Ki = 569.0 nM 6.25
CHEMBL2113435 Ki = 719.0 nM 6.14
CHEMBL2113421 Ki = 2280.0 nM 5.64
CHEMBL2113436 Ki = 8500.0 nM 5.07