Assay Detail
Binding
CHEMBL1218402
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]IP3 from rat recombinant IP3R1 binding core residue (224-604) expressed in chicken DT40 cells by equilibrium competitive binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | DT40 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL2804) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthetic partial agonists reveal key steps in IP3 receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 9.65 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1212943 | — | — | 1 | 9.85 |
| CHEMBL1213158 | — | — | 1 | 9.74 |
| CHEMBL1213159 | — | — | 1 | 9.74 |
| CHEMBL1213160 | — | — | 1 | 9.70 |
| CHEMBL1213163 | — | — | 1 | 9.70 |
| CHEMBL279107 | INS(1,4,5)P3 | — | 1 | 9.68 |
| CHEMBL1213201 | — | — | 1 | 9.66 |
| CHEMBL1213161 | — | — | 1 | 9.48 |
| CHEMBL1213202 | — | — | 1 | 9.28 |
| CHEMBL204385 | ADENOPHOSTIN A | — | 1 | - |
| CHEMBL1213162 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1212943 | — | Kd | = | 0.14 | nM | 9.85 |
| CHEMBL1213158 | — | Kd | = | 0.18 | nM | 9.74 |
| CHEMBL1213159 | — | Kd | = | 0.18 | nM | 9.74 |
| CHEMBL1213160 | — | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL1213163 | — | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL279107 | INS(1,4,5)P3 | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL1213201 | — | Kd | = | 0.22 | nM | 9.66 |
| CHEMBL1213161 | — | Kd | = | 0.33 | nM | 9.48 |
| CHEMBL1213202 | — | Kd | = | 0.52 | nM | 9.28 |
| CHEMBL204385 | ADENOPHOSTIN A | Kd | - | — | - | |
| CHEMBL1213162 | — | Kd | - | — | - |