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Assay Detail

CHEMBL2155058

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

Binding
Displacement of [3H]DPCPX from human A3 adenosine receptor expressed in CHO cells after 60 mins by liquid scintillation counting
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.
Carlsson J, Tosh DK, Phan K, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2012) 3 : 715 -720
PubMed 23342198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 5.86 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151129 1 7.00
CHEMBL2151130 1 6.70
CHEMBL2151126 1 6.70
CHEMBL2151132 1 6.52
CHEMBL2151128 1 6.52
CHEMBL2151125 1 6.52
CHEMBL2151124 1 6.52
CHEMBL2151254 1 6.30
CHEMBL2151131 1 6.22
CHEMBL2151133 1 6.00
CHEMBL2151258 1 6.00
CHEMBL2151117 1 6.00
CHEMBL2151251 1 5.85
CHEMBL2151265 1 5.82
CHEMBL2151256 1 5.82
CHEMBL2151262 1 5.72
CHEMBL2151255 1 5.72
CHEMBL2151260 1 5.66
CHEMBL2151257 1 5.64
CHEMBL2151252 1 5.60
CHEMBL2151249 1 5.58
CHEMBL2151253 1 5.58
CHEMBL2151261 1 5.57
CHEMBL2151127 1 5.51
CHEMBL2151118 1 5.50
CHEMBL2151250 1 5.48
CHEMBL2151264 1 5.34
CHEMBL2151123 1 5.28
CHEMBL2151259 1 5.26
CHEMBL2151120 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151129 Ki = 100.0 nM 7.00
CHEMBL2151130 Ki = 200.0 nM 6.70
CHEMBL2151126 Ki = 200.0 nM 6.70
CHEMBL2151132 Ki = 300.0 nM 6.52
CHEMBL2151128 Ki = 300.0 nM 6.52
CHEMBL2151125 Ki = 300.0 nM 6.52
CHEMBL2151124 Ki = 300.0 nM 6.52
CHEMBL2151254 Ki = 500.0 nM 6.30
CHEMBL2151131 Ki = 600.0 nM 6.22
CHEMBL2151133 Ki = 1000.0 nM 6.00
CHEMBL2151258 Ki = 1000.0 nM 6.00
CHEMBL2151117 Ki = 1000.0 nM 6.00
CHEMBL2151251 Ki = 1400.0 nM 5.85
CHEMBL2151265 Ki = 1500.0 nM 5.82
CHEMBL2151256 Ki = 1500.0 nM 5.82
CHEMBL2151255 Ki = 1900.0 nM 5.72
CHEMBL2151262 Ki = 1900.0 nM 5.72
CHEMBL2151260 Ki = 2200.0 nM 5.66
CHEMBL2151257 Ki = 2300.0 nM 5.64
CHEMBL2151252 Ki = 2500.0 nM 5.60
CHEMBL2151249 Ki = 2600.0 nM 5.58
CHEMBL2151253 Ki = 2600.0 nM 5.58
CHEMBL2151261 Ki = 2700.0 nM 5.57
CHEMBL2151127 Ki = 3100.0 nM 5.51
CHEMBL2151118 Ki = 3200.0 nM 5.50
CHEMBL2151250 Ki = 3300.0 nM 5.48
CHEMBL2151264 Ki = 4600.0 nM 5.34
CHEMBL2151123 Ki = 5300.0 nM 5.28
CHEMBL2151259 Ki = 5500.0 nM 5.26
CHEMBL2151120 Ki = 5900.0 nM 5.23
CHEMBL2151121 Ki = 6300.0 nM 5.20
CHEMBL2151263 Ki = 8300.0 nM 5.08