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Assay Detail

CHEMBL928987

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

Binding
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH.
Bioorg Med Chem Lett (2008) 18 : 1778 -1783
PubMed 18329269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.38 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401895 1 7.22
CHEMBL256123 1 7.17
CHEMBL256124 1 7.17
CHEMBL403845 1 7.14
CHEMBL403846 1 7.11
CHEMBL255911 1 7.06
CHEMBL404864 1 7.02
CHEMBL429125 1 7.00
CHEMBL404863 1 6.92
CHEMBL256332 1 6.92
CHEMBL256331 1 6.85
CHEMBL253317 1 6.82
CHEMBL255699 1 6.75
CHEMBL429850 1 6.70
CHEMBL256548 1 6.57
CHEMBL256547 1 6.57
CHEMBL256327 1 6.32
CHEMBL256546 1 6.27
CHEMBL256125 1 6.22
CHEMBL404739 1 6.19
CHEMBL253528 1 6.13
CHEMBL255649 1 5.96
CHEMBL256755 1 5.92
CHEMBL404740 1 5.89
CHEMBL402781 1 5.85
CHEMBL255861 1 5.82
CHEMBL404744 1 5.68
CHEMBL255859 1 5.66
CHEMBL255860 1 5.37
CHEMBL255267 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401895 Ki = 60.0 nM 7.22
CHEMBL256123 Ki = 68.0 nM 7.17
CHEMBL256124 Ki = 68.0 nM 7.17
CHEMBL403845 Ki = 73.0 nM 7.14
CHEMBL403846 Ki = 78.0 nM 7.11
CHEMBL255911 Ki = 87.0 nM 7.06
CHEMBL404864 Ki = 95.0 nM 7.02
CHEMBL429125 Ki = 100.0 nM 7.00
CHEMBL404863 Ki = 120.0 nM 6.92
CHEMBL256332 Ki = 120.0 nM 6.92
CHEMBL256331 Ki = 140.0 nM 6.85
CHEMBL253317 Ki = 150.0 nM 6.82
CHEMBL255699 Ki = 180.0 nM 6.75
CHEMBL429850 Ki = 200.0 nM 6.70
CHEMBL256548 Ki = 270.0 nM 6.57
CHEMBL256547 Ki = 270.0 nM 6.57
CHEMBL256327 Ki = 480.0 nM 6.32
CHEMBL256546 Ki = 540.0 nM 6.27
CHEMBL256125 Ki = 600.0 nM 6.22
CHEMBL404739 Ki = 650.0 nM 6.19
CHEMBL253528 Ki = 740.0 nM 6.13
CHEMBL255649 Ki = 1100.0 nM 5.96
CHEMBL256755 Ki = 1200.0 nM 5.92
CHEMBL404740 Ki = 1300.0 nM 5.89
CHEMBL402781 Ki = 1400.0 nM 5.85
CHEMBL255861 Ki = 1500.0 nM 5.82
CHEMBL404744 Ki = 2100.0 nM 5.68
CHEMBL255859 Ki = 2200.0 nM 5.66
CHEMBL255860 Ki = 4300.0 nM 5.37
CHEMBL255267 Ki = 9700.0 nM 5.01
CHEMBL402904 Ki = 25000.0 nM 4.60