Assay Detail
Functional
CHEMBL2014010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X3 receptor expressed in RLE cells assessed as inhibition of (alpha,beta)me-ATP-induced intracellular calcium level by FLIPR assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RLE |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of P2X3 selective antagonists for the treatment of chronic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.42 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2011127 | — | — | 1 | 7.66 |
| CHEMBL2011126 | — | — | 1 | 7.62 |
| CHEMBL2011125 | — | — | 1 | 7.62 |
| CHEMBL2011123 | — | — | 1 | 7.42 |
| CHEMBL2011112 | — | — | 1 | 7.21 |
| CHEMBL2011118 | — | — | 1 | 7.19 |
| CHEMBL2011116 | — | — | 1 | 7.17 |
| CHEMBL2011120 | — | — | 1 | 7.16 |
| CHEMBL2011122 | — | — | 1 | 6.94 |
| CHEMBL2011121 | — | — | 1 | 6.67 |
| CHEMBL2010931 | — | — | 1 | 6.59 |
| CHEMBL2011111 | — | — | 1 | 6.58 |
| CHEMBL2010933 | — | — | 1 | 6.57 |
| CHEMBL2010930 | — | — | 1 | 6.49 |
| CHEMBL2011115 | — | — | 1 | 6.49 |
| CHEMBL2011102 | — | — | 1 | 6.40 |
| CHEMBL2011103 | — | — | 1 | 6.36 |
| CHEMBL2011109 | — | — | 1 | 6.36 |
| CHEMBL2011124 | — | — | 1 | 6.28 |
| CHEMBL2010929 | — | — | 1 | 6.21 |
| CHEMBL2011117 | — | — | 1 | 6.21 |
| CHEMBL2011114 | — | — | 1 | 5.90 |
| CHEMBL2011108 | — | — | 1 | 5.88 |
| CHEMBL2010928 | — | — | 1 | 5.87 |
| CHEMBL2011107 | — | — | 1 | 5.78 |
| CHEMBL2010932 | — | — | 1 | 5.71 |
| CHEMBL2011110 | — | — | 1 | 5.69 |
| CHEMBL2011119 | — | — | 1 | 5.60 |
| CHEMBL2011113 | — | — | 1 | 5.38 |
| CHEMBL2011104 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2011127 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2011126 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2011125 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2011123 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2011112 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2011118 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2011116 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2011120 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2011122 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL2011121 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL2010931 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL2011111 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL2010933 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL2010930 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL2011115 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL2011102 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL2011103 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2011109 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL2011124 | — | IC50 | = | 521.0 | nM | 6.28 |
| CHEMBL2010929 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL2011117 | — | IC50 | = | 613.0 | nM | 6.21 |
| CHEMBL2011114 | — | IC50 | = | 1271.0 | nM | 5.90 |
| CHEMBL2011108 | — | IC50 | = | 1311.0 | nM | 5.88 |
| CHEMBL2010928 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL2011107 | — | IC50 | = | 1665.0 | nM | 5.78 |
| CHEMBL2010932 | — | IC50 | = | 1947.0 | nM | 5.71 |
| CHEMBL2011110 | — | IC50 | = | 2057.0 | nM | 5.69 |
| CHEMBL2011119 | — | IC50 | = | 2523.0 | nM | 5.60 |
| CHEMBL2011113 | — | IC50 | = | 4214.0 | nM | 5.38 |
| CHEMBL2011104 | — | IC50 | = | 5689.0 | nM | 5.25 |
| CHEMBL2011106 | — | IC50 | = | 13950.0 | nM | 4.86 |
| CHEMBL2011105 | — | IC50 | > | 30000.0 | nM | - |