Assay Detail
Functional
CHEMBL855905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at rat IP3 type 1 receptor expressed in DT40 cell assessed as calcium ion mobilization
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | DT40 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL2804) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP3 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 8.23 | 8.68 |
| Inhibition | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1161890 | — | — | 2 | 8.68 |
| CHEMBL204385 | ADENOPHOSTIN A | — | 2 | 8.68 |
| CHEMBL1161892 | — | — | 2 | 8.57 |
| CHEMBL1161891 | — | — | 2 | 8.55 |
| CHEMBL279107 | INS(1,4,5)P3 | — | 2 | 7.61 |
| CHEMBL1161893 | — | — | 2 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1161890 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL204385 | ADENOPHOSTIN A | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1161892 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1161891 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL279107 | INS(1,4,5)P3 | EC50 | = | 24.8 | nM | 7.61 |
| CHEMBL1161893 | — | EC50 | = | 53.3 | nM | 7.27 |
| CHEMBL279107 | INS(1,4,5)P3 | Inhibition | = | 78.0 | % | - |
| CHEMBL1161893 | — | Inhibition | = | 79.0 | % | - |
| CHEMBL1161892 | — | Inhibition | = | 79.0 | % | - |
| CHEMBL1161891 | — | Inhibition | = | 76.0 | % | - |
| CHEMBL1161890 | — | Inhibition | = | 77.0 | % | - |
| CHEMBL204385 | ADENOPHOSTIN A | Inhibition | = | 76.0 | % | - |