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Assay Detail

CHEMBL3706155

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Binding
Radioligand Binding Assay: human or rat P2X7-1321N1 cells were collected and frozen @ −80° C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 μl:10 μl compound (10×)+(b) 40 μl tracer (2.5x)+50 μl membrane (2×). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2008, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4° C. The assay was terminated by filtration (GF/B filters pre-soaked with 0.3% PEI) and washed with washing buffer (Tris-HCl 50 mM).
ChEMBL ↗
82
Total Activities
80
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type P2X7-1321N1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

P2X purinoceptor 7 (CHEMBL4805) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

P2X7 modulators
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 82 7.39 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3674094 — — 1 8.20
CHEMBL3674097 — — 1 8.10
CHEMBL3674100 — — 1 8.10
CHEMBL3674126 — — 1 8.10
CHEMBL3674055 — — 2 8.02
CHEMBL3674103 — — 1 8.00
CHEMBL3674107 — — 1 7.94
CHEMBL3674132 — — 1 7.90
CHEMBL3674131 — — 1 7.90
CHEMBL3674122 — — 1 7.90
CHEMBL3674090 — — 1 7.90
CHEMBL3674086 — — 1 7.90
CHEMBL3674042 — — 1 7.81
CHEMBL3674087 — — 1 7.80
CHEMBL3674077 — — 1 7.80
CHEMBL3674061 — — 1 7.79
CHEMBL3674116 — — 1 7.76
CHEMBL3674074 — — 1 7.75
CHEMBL3674119 — — 1 7.70
CHEMBL3674135 — — 1 7.70
CHEMBL3674134 — — 1 7.70
CHEMBL3674050 — — 1 7.70
CHEMBL3674082 — — 1 7.65
CHEMBL3674051 — — 1 7.60
CHEMBL3674093 — — 1 7.60
CHEMBL3674081 — — 1 7.60
CHEMBL3674052 — — 1 7.60
CHEMBL3674099 — — 1 7.60
CHEMBL3674125 — — 1 7.60
CHEMBL3674108 — — 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3674094 — Ki = 6.3 nM 8.20
CHEMBL3674126 — Ki = 7.9 nM 8.10
CHEMBL3674100 — Ki = 7.9 nM 8.10
CHEMBL3674097 — Ki = 7.9 nM 8.10
CHEMBL3674055 — Ki = 9.5 nM 8.02
CHEMBL3674055 — Ki = 9.5 nM 8.02
CHEMBL3674103 — Ki = 10.0 nM 8.00
CHEMBL3674107 — Ki = 11.5 nM 7.94
CHEMBL3674132 — Ki = 12.6 nM 7.90
CHEMBL3674131 — Ki = 12.6 nM 7.90
CHEMBL3674122 — Ki = 12.6 nM 7.90
CHEMBL3674090 — Ki = 12.6 nM 7.90
CHEMBL3674086 — Ki = 12.6 nM 7.90
CHEMBL3674042 — Ki = 15.4 nM 7.81
CHEMBL3674087 — Ki = 15.8 nM 7.80
CHEMBL3674077 — Ki = 15.8 nM 7.80
CHEMBL3674061 — Ki = 16.4 nM 7.79
CHEMBL3674116 — Ki = 17.4 nM 7.76
CHEMBL3674074 — Ki = 17.8 nM 7.75
CHEMBL3674135 — Ki = 20.0 nM 7.70
CHEMBL3674134 — Ki = 20.0 nM 7.70
CHEMBL3674119 — Ki = 20.0 nM 7.70
CHEMBL3674050 — Ki = 20.0 nM 7.70
CHEMBL3674082 — Ki = 22.4 nM 7.65
CHEMBL3674125 — Ki = 25.1 nM 7.60
CHEMBL3674081 — Ki = 25.1 nM 7.60
CHEMBL3674137 — Ki = 25.1 nM 7.60
CHEMBL3674108 — Ki = 25.1 nM 7.60
CHEMBL3674052 — Ki = 25.1 nM 7.60
CHEMBL3674093 — Ki = 25.1 nM 7.60
CHEMBL3674051 — Ki = 25.1 nM 7.60
CHEMBL3674099 — Ki = 25.1 nM 7.60
CHEMBL3674056 — Ki = 26.6 nM 7.58
CHEMBL3674056 — Ki = 26.6 nM 7.58
CHEMBL3674044 — Ki = 30.9 nM 7.51
CHEMBL3674096 — Ki = 31.6 nM 7.50
CHEMBL3674128 — Ki = 31.6 nM 7.50
CHEMBL3674139 — Ki = 31.6 nM 7.50
CHEMBL3674129 — Ki = 31.6 nM 7.50
CHEMBL3674105 — Ki = 31.6 nM 7.50
CHEMBL3674112 — Ki = 31.6 nM 7.50
CHEMBL3674102 — Ki = 31.6 nM 7.50
CHEMBL3674075 — Ki = 37.2 nM 7.43
CHEMBL3674045 — Ki = 37.2 nM 7.43
CHEMBL3674140 — Ki = 39.8 nM 7.40
CHEMBL3674070 — Ki = 39.8 nM 7.40
CHEMBL3674089 — Ki = 39.8 nM 7.40
CHEMBL3674053 — Ki = 39.8 nM 7.40
CHEMBL3674121 — Ki = 39.8 nM 7.40
CHEMBL3639729 — Ki = 39.8 nM 7.40