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Assay Detail

CHEMBL644656

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Binding
Binding affinity against human Adenosine A2a receptor (hA2a)
42
Total Activities
42
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 A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
Guba W, Nettekoven M, Püllmann B, Riemer C, Schmitt S.
Bioorg Med Chem Lett (2004) 14 : 3307 -3312
PubMed 15149696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.74 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17127 SCH-58261 1 9.22
CHEMBL113142 ZM-241385 1 9.10
CHEMBL112773 1 8.70
CHEMBL113967 1 8.70
CHEMBL323945 1 8.52
CHEMBL110069 1 8.52
CHEMBL112631 1 8.52
CHEMBL110074 1 8.40
CHEMBL323621 1 8.40
CHEMBL420307 1 8.30
CHEMBL110698 1 8.22
CHEMBL324077 1 8.22
CHEMBL332718 1 8.10
CHEMBL325237 1 8.05
CHEMBL325350 1 8.05
CHEMBL109499 1 7.96
CHEMBL320349 1 7.92
CHEMBL113228 1 7.85
CHEMBL113542 1 7.82
CHEMBL110047 1 7.80
CHEMBL324591 1 7.77
CHEMBL113541 1 7.64
CHEMBL114185 1 7.57
CHEMBL113376 1 7.57
CHEMBL109845 1 7.57
CHEMBL112195 1 7.46
CHEMBL112897 1 7.40
CHEMBL113009 1 7.36
CHEMBL112740 1 7.30
CHEMBL419191 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17127 SCH-58261 Ki = 0.6 nM 9.22
CHEMBL113142 ZM-241385 Ki = 0.8 nM 9.10
CHEMBL113967 Ki = 2.0 nM 8.70
CHEMBL112773 Ki = 2.0 nM 8.70
CHEMBL323945 Ki = 3.0 nM 8.52
CHEMBL110069 Ki = 3.0 nM 8.52
CHEMBL112631 Ki = 3.0 nM 8.52
CHEMBL110074 Ki = 4.0 nM 8.40
CHEMBL323621 Ki = 4.0 nM 8.40
CHEMBL420307 Ki = 5.0 nM 8.30
CHEMBL110698 Ki = 6.0 nM 8.22
CHEMBL324077 Ki = 6.0 nM 8.22
CHEMBL332718 Ki = 8.0 nM 8.10
CHEMBL325237 Ki = 9.0 nM 8.05
CHEMBL325350 Ki = 9.0 nM 8.05
CHEMBL109499 Ki = 11.0 nM 7.96
CHEMBL320349 Ki = 12.0 nM 7.92
CHEMBL113228 Ki = 14.0 nM 7.85
CHEMBL113542 Ki = 15.0 nM 7.82
CHEMBL110047 Ki = 16.0 nM 7.80
CHEMBL324591 Ki = 17.0 nM 7.77
CHEMBL113541 Ki = 23.0 nM 7.64
CHEMBL113376 Ki = 27.0 nM 7.57
CHEMBL109845 Ki = 27.0 nM 7.57
CHEMBL114185 Ki = 27.0 nM 7.57
CHEMBL112195 Ki = 35.0 nM 7.46
CHEMBL112897 Ki = 40.0 nM 7.40
CHEMBL113009 Ki = 44.0 nM 7.36
CHEMBL112740 Ki = 50.0 nM 7.30
CHEMBL419191 Ki = 57.0 nM 7.24
CHEMBL113412 Ki = 57.0 nM 7.24
CHEMBL325646 Ki = 57.0 nM 7.24
CHEMBL325993 Ki = 62.0 nM 7.21
CHEMBL110646 Ki = 61.0 nM 7.21
CHEMBL323754 Ki = 73.0 nM 7.14
CHEMBL432624 Ki = 76.0 nM 7.12
CHEMBL113468 Ki = 76.0 nM 7.12
CHEMBL114405 Ki = 104.0 nM 6.98
CHEMBL112249 Ki = 192.0 nM 6.72
CHEMBL109753 Ki = 190.0 nM 6.72
CHEMBL433162 Ki = 197.0 nM 6.71
CHEMBL113189 Ki = 277.0 nM 6.56