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Assay Detail

CHEMBL3706099

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Binding
Radioligand Binding: Human or rat P2X7-1321N1 cells were collected and frozen @-80.degree. C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 .mu.l:10 .mu.l compound (10.times.)+(b) 40 .mu.l tracer (2.5.times.)+50 .mu.l membrane (2.times.). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2009, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4.degree. 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 ↗
40
Total Activities
40
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

5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocines as P2X7 modulators
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 7.69 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3697551 — — 1 8.40
CHEMBL3697552 — — 1 8.20
CHEMBL3697516 — — 1 8.00
CHEMBL3697548 — — 1 8.00
CHEMBL3697537 — — 1 8.00
CHEMBL3697527 — — 1 7.98
CHEMBL3697528 — — 1 7.97
CHEMBL3697531 — — 1 7.90
CHEMBL3697543 — — 1 7.90
CHEMBL3697519 — — 1 7.90
CHEMBL3697535 — — 1 7.90
CHEMBL3697534 — — 1 7.90
CHEMBL3697513 — — 1 7.90
CHEMBL3697532 — — 1 7.90
CHEMBL3697515 — — 1 7.90
CHEMBL3697533 — — 1 7.89
CHEMBL3697521 — — 1 7.86
CHEMBL3697536 — — 1 7.80
CHEMBL3697540 — — 1 7.80
CHEMBL3697520 — — 1 7.76
CHEMBL3697512 — — 1 7.70
CHEMBL3697539 — — 1 7.70
CHEMBL3697530 — — 1 7.66
CHEMBL3697550 — — 1 7.66
CHEMBL3697523 — — 1 7.62
CHEMBL3697545 — — 1 7.60
CHEMBL3697544 — — 1 7.60
CHEMBL3697529 — — 1 7.60
CHEMBL6067665 — — 1 7.52
CHEMBL3697542 — — 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3697551 — Ki = 4.0 nM 8.40
CHEMBL3697552 — Ki = 6.3 nM 8.20
CHEMBL3697548 — Ki = 10.0 nM 8.00
CHEMBL3697537 — Ki = 10.0 nM 8.00
CHEMBL3697516 — Ki = 10.0 nM 8.00
CHEMBL3697527 — Ki = 10.5 nM 7.98
CHEMBL3697528 — Ki = 10.7 nM 7.97
CHEMBL3697534 — Ki = 12.6 nM 7.90
CHEMBL3697515 — Ki = 12.6 nM 7.90
CHEMBL3697532 — Ki = 12.6 nM 7.90
CHEMBL3697513 — Ki = 12.6 nM 7.90
CHEMBL3697535 — Ki = 12.6 nM 7.90
CHEMBL3697519 — Ki = 12.6 nM 7.90
CHEMBL3697543 — Ki = 12.6 nM 7.90
CHEMBL3697531 — Ki = 12.6 nM 7.90
CHEMBL3697533 — Ki = 12.9 nM 7.89
CHEMBL3697521 — Ki = 13.8 nM 7.86
CHEMBL3697536 — Ki = 15.8 nM 7.80
CHEMBL3697540 — Ki = 15.8 nM 7.80
CHEMBL3697520 — Ki = 17.4 nM 7.76
CHEMBL3697512 — Ki = 20.0 nM 7.70
CHEMBL3697539 — Ki = 20.0 nM 7.70
CHEMBL3697530 — Ki = 21.9 nM 7.66
CHEMBL3697550 — Ki = 21.9 nM 7.66
CHEMBL3697523 — Ki = 24.0 nM 7.62
CHEMBL3697545 — Ki = 25.1 nM 7.60
CHEMBL3697544 — Ki = 25.1 nM 7.60
CHEMBL3697529 — Ki = 25.1 nM 7.60
CHEMBL6067665 — Ki = 30.4 nM 7.52
CHEMBL3697542 — Ki = 31.6 nM 7.50
CHEMBL3697526 — Ki = 35.5 nM 7.45
CHEMBL3697547 — Ki = 35.5 nM 7.45
CHEMBL3697538 — Ki = 39.8 nM 7.40
CHEMBL3697541 — Ki = 39.8 nM 7.40
CHEMBL3697546 — Ki = 39.8 nM 7.40
CHEMBL3697511 — Ki = 39.8 nM 7.40
CHEMBL3697522 — Ki = 50.1 nM 7.30
CHEMBL3697509 — Ki = 50.1 nM 7.30
CHEMBL3697549 — Ki = 125.9 nM 6.90
CHEMBL3697517 — Ki = 398.1 nM 6.40