Assay Detail
Binding
CHEMBL4615154
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control
66
Total Activities
65
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 65 | 6.18 | 7.72 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL536151 | IMD-0354 | 1.0 | 2 | 7.72 |
| CHEMBL2338696 | — | — | 1 | 7.64 |
| CHEMBL2179173 | — | — | 1 | 7.53 |
| CHEMBL4640175 | — | — | 1 | 7.50 |
| CHEMBL2088014 | — | — | 1 | 7.42 |
| CHEMBL2179174 | — | — | 1 | 7.30 |
| CHEMBL2338695 | — | — | 1 | 7.24 |
| CHEMBL4644398 | — | — | 1 | 7.15 |
| CHEMBL2088011 | — | — | 1 | 7.12 |
| CHEMBL461542 | — | — | 1 | 7.11 |
| CHEMBL589733 | — | — | 1 | 7.04 |
| CHEMBL2088009 | — | — | 1 | 6.76 |
| CHEMBL2088012 | — | — | 1 | 6.70 |
| CHEMBL4637528 | — | — | 1 | 6.66 |
| CHEMBL2313115 | — | — | 1 | 6.63 |
| CHEMBL1253351 | — | — | 1 | 6.63 |
| CHEMBL2178702 | — | — | 1 | 6.49 |
| CHEMBL4648128 | — | — | 1 | 6.47 |
| CHEMBL2338686 | — | — | 1 | 6.47 |
| CHEMBL2313133 | — | — | 1 | 6.36 |
| CHEMBL190141 | — | — | 1 | 6.30 |
| CHEMBL2179168 | — | — | 1 | 6.28 |
| CHEMBL2179170 | — | — | 1 | 6.25 |
| CHEMBL4639803 | — | — | 1 | 6.18 |
| CHEMBL2313119 | — | — | 1 | 6.12 |
| CHEMBL3628655 | — | — | 1 | 6.06 |
| CHEMBL4634436 | — | — | 1 | 6.04 |
| CHEMBL2312822 | — | — | 1 | 6.04 |
| CHEMBL2104794 | SALFLUVERINE | 2.0 | 1 | 5.89 |
| CHEMBL2179166 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL536151 | IMD-0354 | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL2338696 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL2179173 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL4640175 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL2088014 | — | IC50 | = | 38.3 | nM | 7.42 |
| CHEMBL2179174 | — | IC50 | = | 50.5 | nM | 7.30 |
| CHEMBL2338695 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4644398 | — | IC50 | = | 70.6 | nM | 7.15 |
| CHEMBL2088011 | — | IC50 | = | 75.6 | nM | 7.12 |
| CHEMBL461542 | — | IC50 | = | 76.9 | nM | 7.11 |
| CHEMBL589733 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2088009 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL2088012 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4637528 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL1253351 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL2313115 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL2178702 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL4648128 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL2338686 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL2313133 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL190141 | — | IC50 | = | 496.0 | nM | 6.30 |
| CHEMBL2179168 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL2179170 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL4639803 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL2313119 | — | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL3628655 | — | IC50 | = | 869.0 | nM | 6.06 |
| CHEMBL2312822 | — | IC50 | = | 907.0 | nM | 6.04 |
| CHEMBL4634436 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL2104794 | SALFLUVERINE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2179166 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL2313134 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL2313116 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4644509 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL2313113 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL2313122 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL4641171 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL4643605 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL2313128 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL4641185 | — | IC50 | = | 4060.0 | nM | 5.39 |
| CHEMBL4647253 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL4637064 | — | IC50 | = | 4910.0 | nM | 5.31 |
| CHEMBL4636258 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL4638155 | — | IC50 | = | 7180.0 | nM | 5.14 |
| CHEMBL4636039 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL4635672 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4647322 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4567302 | — | IC50 | = | 9930.0 | nM | 5.00 |
| CHEMBL4632715 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4646767 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL536151 | IMD-0354 | Inhibition | - | % | - |