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Assay Detail

CHEMBL939996

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Binding
Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in CHO cells
ChEMBL ↗
69
Total Activities
68
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 A2a (CHEMBL251) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
Stefanachi A, Brea JM, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Vidal B, Carotti A.
Bioorg Med Chem (2008) 16 : 2852 -2869
PubMed 18226909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 69 6.35 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259870 — — 1 7.42
CHEMBL408048 — — 1 7.31
CHEMBL258979 — — 1 7.13
CHEMBL258978 — — 1 7.03
CHEMBL262332 — — 1 6.97
CHEMBL411075 — — 1 6.94
CHEMBL260051 — — 1 6.94
CHEMBL412063 — — 1 6.88
CHEMBL260433 — — 1 6.82
CHEMBL261792 — — 1 6.81
CHEMBL260693 — — 1 6.81
CHEMBL412293 — — 1 6.80
CHEMBL259057 — — 1 6.79
CHEMBL259529 — — 1 6.77
CHEMBL260221 — — 1 6.76
CHEMBL411720 — — 1 6.76
CHEMBL440418 — — 1 6.74
CHEMBL408185 — — 2 6.68
CHEMBL411275 — — 1 6.65
CHEMBL259104 — — 1 6.62
CHEMBL259871 — — 1 6.62
CHEMBL409514 — — 1 6.59
CHEMBL407179 — — 1 6.58
CHEMBL261068 — — 1 6.57
CHEMBL258810 — — 1 6.52
CHEMBL259581 — — 1 6.50
CHEMBL259733 — — 1 6.49
CHEMBL258568 — — 1 6.49
CHEMBL412112 — — 1 6.49
CHEMBL259360 — — 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259870 — Ki = 38.02 nM 7.42
CHEMBL408048 — Ki = 48.98 nM 7.31
CHEMBL258979 — Ki = 74.13 nM 7.13
CHEMBL258978 — Ki = 93.33 nM 7.03
CHEMBL262332 — Ki = 107.15 nM 6.97
CHEMBL411075 — Ki = 114.82 nM 6.94
CHEMBL260051 — Ki = 114.82 nM 6.94
CHEMBL412063 — Ki = 131.83 nM 6.88
CHEMBL260433 — Ki = 151.36 nM 6.82
CHEMBL261792 — Ki = 154.88 nM 6.81
CHEMBL260693 — Ki = 154.88 nM 6.81
CHEMBL412293 — Ki = 158.49 nM 6.80
CHEMBL259057 — Ki = 162.18 nM 6.79
CHEMBL259529 — Ki = 169.82 nM 6.77
CHEMBL411720 — Ki = 173.78 nM 6.76
CHEMBL260221 — Ki = 173.78 nM 6.76
CHEMBL440418 — Ki = 181.97 nM 6.74
CHEMBL408185 — Ki = 208.93 nM 6.68
CHEMBL411275 — Ki = 223.87 nM 6.65
CHEMBL259104 — Ki = 239.88 nM 6.62
CHEMBL259871 — Ki = 239.88 nM 6.62
CHEMBL409514 — Ki = 257.04 nM 6.59
CHEMBL407179 — Ki = 263.03 nM 6.58
CHEMBL261068 — Ki = 269.15 nM 6.57
CHEMBL258810 — Ki = 302.0 nM 6.52
CHEMBL259581 — Ki = 316.23 nM 6.50
CHEMBL258568 — Ki = 323.59 nM 6.49
CHEMBL412112 — Ki = 323.59 nM 6.49
CHEMBL259360 — Ki = 323.59 nM 6.49
CHEMBL259733 — Ki = 323.59 nM 6.49
CHEMBL409726 — Ki = 354.81 nM 6.45
CHEMBL262333 — Ki = 354.81 nM 6.45
CHEMBL410297 — Ki = 354.81 nM 6.45
CHEMBL260692 — Ki = 389.05 nM 6.41
CHEMBL429512 — Ki = 398.11 nM 6.40
CHEMBL261056 — Ki = 398.11 nM 6.40
CHEMBL261212 — Ki = 398.11 nM 6.40
CHEMBL259151 — Ki = 407.38 nM 6.39
CHEMBL263895 — Ki = 416.87 nM 6.38
CHEMBL259105 — Ki = 426.58 nM 6.37
CHEMBL259580 — Ki = 467.74 nM 6.33
CHEMBL409443 — Ki = 478.63 nM 6.32
CHEMBL428604 — Ki = 562.34 nM 6.25
CHEMBL260180 — Ki = 588.84 nM 6.23
CHEMBL409725 — Ki = 616.6 nM 6.21
CHEMBL407202 — Ki = 630.96 nM 6.20
CHEMBL258948 — Ki = 645.65 nM 6.19
CHEMBL409481 — Ki = 691.83 nM 6.16
CHEMBL259056 — Ki = 707.95 nM 6.15
CHEMBL260495 — Ki = 707.95 nM 6.15