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Assay Detail

CHEMBL1037718

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Binding
Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells
ChEMBL ↗
339
Total Activities
186
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 Intermediate

Target

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

Publication

Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
Michielan L, Bolcato C, Federico S, Cacciari B, Bacilieri M, Klotz KN, Kachler S, Pastorin G, Cardin R, Sperduti A, Spalluto G, Moro S.
Bioorg Med Chem (2009) 17 : 5259 -5274
PubMed 19501513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 339 8.04 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348975 — — 2 9.85
CHEMBL145767 — — 2 9.85
CHEMBL168018 — — 2 9.82
CHEMBL324735 — — 2 9.80
CHEMBL352796 — — 2 9.74
CHEMBL329791 — — 2 9.70
CHEMBL352073 — — 2 9.70
CHEMBL349240 — — 2 9.68
CHEMBL166684 — — 2 9.68
CHEMBL165224 — — 2 9.62
CHEMBL578224 — — 2 9.60
CHEMBL165083 — — 2 9.57
CHEMBL167753 — — 2 9.54
CHEMBL165778 — — 2 9.54
CHEMBL352345 — — 2 9.52
CHEMBL166301 — — 2 9.52
CHEMBL351285 — — 2 9.51
CHEMBL330286 — — 2 9.49
CHEMBL164905 — — 2 9.47
CHEMBL165560 — — 2 9.47
CHEMBL572765 — — 2 9.47
CHEMBL165600 — — 2 9.43
CHEMBL344501 — — 2 9.40
CHEMBL350261 — — 2 9.40
CHEMBL351075 — — 2 9.40
CHEMBL424161 — — 2 9.37
CHEMBL354161 — — 2 9.37
CHEMBL350205 — — 2 9.35
CHEMBL348925 — — 2 9.34
CHEMBL577183 — — 2 9.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL145767 — Ki = 0.1413 nM 9.85
CHEMBL348975 — Ki = 0.14 nM 9.85
CHEMBL348975 — Ki = 0.1413 nM 9.85
CHEMBL145767 — Ki = 0.14 nM 9.85
CHEMBL168018 — Ki = 0.15 nM 9.82
CHEMBL168018 — Ki = 0.1514 nM 9.82
CHEMBL324735 — Ki = 0.16 nM 9.80
CHEMBL324735 — Ki = 0.1585 nM 9.80
CHEMBL352796 — Ki = 0.18 nM 9.74
CHEMBL352796 — Ki = 0.182 nM 9.74
CHEMBL329791 — Ki = 0.2 nM 9.70
CHEMBL329791 — Ki = 0.1995 nM 9.70
CHEMBL352073 — Ki = 0.2 nM 9.70
CHEMBL352073 — Ki = 0.1995 nM 9.70
CHEMBL166684 — Ki = 0.2089 nM 9.68
CHEMBL349240 — Ki = 0.2089 nM 9.68
CHEMBL349240 — Ki = 0.21 nM 9.68
CHEMBL166684 — Ki = 0.21 nM 9.68
CHEMBL165224 — Ki = 0.24 nM 9.62
CHEMBL165224 — Ki = 0.2399 nM 9.62
CHEMBL578224 — Ki = 0.25 nM 9.60
CHEMBL578224 — Ki = 0.2512 nM 9.60
CHEMBL165083 — Ki = 0.27 nM 9.57
CHEMBL165083 — Ki = 0.2692 nM 9.57
CHEMBL167753 — Ki = 0.2884 nM 9.54
CHEMBL165778 — Ki = 0.29 nM 9.54
CHEMBL165778 — Ki = 0.2884 nM 9.54
CHEMBL167753 — Ki = 0.29 nM 9.54
CHEMBL166301 — Ki = 0.3 nM 9.52
CHEMBL352345 — Ki = 0.3 nM 9.52
CHEMBL166301 — Ki = 0.302 nM 9.52
CHEMBL352345 — Ki = 0.302 nM 9.52
CHEMBL351285 — Ki = 0.31 nM 9.51
CHEMBL351285 — Ki = 0.309 nM 9.51
CHEMBL330286 — Ki = 0.32 nM 9.49
CHEMBL330286 — Ki = 0.3236 nM 9.49
CHEMBL165560 — Ki = 0.34 nM 9.47
CHEMBL165560 — Ki = 0.3388 nM 9.47
CHEMBL164905 — Ki = 0.3388 nM 9.47
CHEMBL572765 — Ki = 0.3388 nM 9.47
CHEMBL164905 — Ki = 0.34 nM 9.47
CHEMBL572765 — Ki = 0.34 nM 9.47
CHEMBL165600 — Ki = 0.3715 nM 9.43
CHEMBL165600 — Ki = 0.37 nM 9.43
CHEMBL344501 — Ki = 0.3981 nM 9.40
CHEMBL351075 — Ki = 0.3981 nM 9.40
CHEMBL350261 — Ki = 0.3981 nM 9.40
CHEMBL344501 — Ki = 0.4 nM 9.40
CHEMBL351075 — Ki = 0.4 nM 9.40
CHEMBL350261 — Ki = 0.4 nM 9.40