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Assay Detail

CHEMBL639745

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

Binding
Displacement of [3H]DPCPX from Adenosine A1 receptor of rat cortical membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
van Tilburg EW, van der Klein PA, de Groote M, Beukers MW, IJzerman AP.
Bioorg Med Chem Lett (2001) 11 : 2017 -2019
PubMed 11454470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.08 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62078 1 7.75
CHEMBL60027 1 7.66
CHEMBL305322 1 7.50
CHEMBL61836 1 7.48
CHEMBL294175 1 7.44
CHEMBL60334 1 7.41
CHEMBL61381 1 7.24
CHEMBL293437 1 7.23
CHEMBL60156 1 7.12
CHEMBL61222 1 7.07
CHEMBL59978 1 6.78
CHEMBL293635 1 5.87
CHEMBL62075 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62078 Ki = 18.0 nM 7.75
CHEMBL60027 Ki = 22.0 nM 7.66
CHEMBL305322 Ki = 32.0 nM 7.50
CHEMBL61836 Ki = 33.0 nM 7.48
CHEMBL294175 Ki = 36.0 nM 7.44
CHEMBL60334 Ki = 39.0 nM 7.41
CHEMBL61381 Ki = 58.0 nM 7.24
CHEMBL293437 Ki = 59.0 nM 7.23
CHEMBL60156 Ki = 76.0 nM 7.12
CHEMBL61222 Ki = 86.0 nM 7.07
CHEMBL59978 Ki = 165.0 nM 6.78
CHEMBL293635 Ki = 1360.0 nM 5.87
CHEMBL62075 Ki = 3000.0 nM 5.52