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Assay Detail

CHEMBL640468

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

Binding
Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the presence of 1 mM of GTP
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 5.88 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2070507 1 6.76
CHEMBL2113421 1 6.34
CHEMBL2113431 1 6.32
CHEMBL464859 NECA 1 6.28
CHEMBL261482 1 6.23
CHEMBL606095 1 6.09
CHEMBL2070399 1 6.05
CHEMBL2113434 1 5.71
CHEMBL2113435 1 5.63
CHEMBL1235128 1 5.40
CHEMBL2070508 1 5.31
CHEMBL519809 1 5.17
CHEMBL2113436 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2070507 Ki = 172.0 nM 6.76
CHEMBL2113421 Ki = 459.0 nM 6.34
CHEMBL2113431 Ki = 478.0 nM 6.32
CHEMBL464859 NECA Ki = 530.0 nM 6.28
CHEMBL261482 Ki = 585.0 nM 6.23
CHEMBL606095 Ki = 804.0 nM 6.09
CHEMBL2070399 Ki = 890.0 nM 6.05
CHEMBL2113434 Ki = 1960.0 nM 5.71
CHEMBL2113435 Ki = 2349.0 nM 5.63
CHEMBL1235128 Ki = 3960.0 nM 5.40
CHEMBL2070508 Ki = 4900.0 nM 5.31
CHEMBL519809 Ki = 6840.0 nM 5.17
CHEMBL2113436 Ki = 6946.0 nM 5.16