Assay Detail
Binding
CHEMBL3858376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubated for 30 mins followed by agonist addition measured after 180 sec by calcium-4 dye based FLIPR assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3895947 | — | — | 1 | 8.40 |
| CHEMBL3906769 | — | — | 1 | 8.40 |
| CHEMBL3901310 | — | — | 1 | 8.30 |
| CHEMBL3947089 | — | — | 1 | 8.05 |
| CHEMBL3913899 | — | — | 1 | 8.05 |
| CHEMBL3911413 | — | — | 1 | 8.00 |
| CHEMBL3956010 | — | — | 1 | 7.92 |
| CHEMBL3962858 | — | — | 1 | 7.85 |
| CHEMBL3955145 | — | — | 1 | 7.82 |
| CHEMBL3919300 | — | — | 1 | 7.55 |
| CHEMBL3910372 | — | — | 1 | 7.52 |
| CHEMBL3960075 | — | — | 1 | 7.47 |
| CHEMBL3901705 | — | — | 1 | 7.47 |
| CHEMBL3904907 | — | — | 1 | 7.17 |
| CHEMBL3898553 | — | — | 1 | 7.11 |
| CHEMBL3914545 | — | — | 1 | 7.11 |
| CHEMBL3907060 | — | — | 1 | 7.05 |
| CHEMBL3948603 | — | — | 1 | 6.94 |
| CHEMBL3894854 | — | — | 1 | 6.06 |
| CHEMBL3929261 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3895947 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3906769 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3901310 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3947089 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3913899 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3911413 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3956010 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3962858 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3955145 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3919300 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3910372 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3960075 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3901705 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3904907 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3898553 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3914545 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3907060 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3948603 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3894854 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3929261 | — | IC50 | = | 3538.0 | nM | 5.45 |