Assay Detail
Binding
CHEMBL815029
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Dissociation constant using IP3-binding domain (IBD) of human Type 1 inositol 1,4,5-trisphosphate receptor
10
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL4046) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hydrophobic modifications at 1-phosphate of inositol 1,4,5-trisphosphate analogues enhance receptor binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 10 | 6.41 | 8.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL172534 | — | — | 1 | 8.93 |
| CHEMBL434103 | — | — | 2 | 6.85 |
| CHEMBL169923 | — | — | 2 | 6.80 |
| CHEMBL352326 | — | — | 2 | 6.77 |
| CHEMBL279107 | INS(1,4,5)P3 | — | 1 | 6.58 |
| CHEMBL369479 | — | — | 1 | 6.21 |
| CHEMBL297235 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL172534 | — | Kd | = | 1.17 | nM | 8.93 |
| CHEMBL434103 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL169923 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL352326 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL279107 | INS(1,4,5)P3 | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL369479 | — | Kd | = | 620.0 | nM | 6.21 |
| CHEMBL297235 | — | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL434103 | — | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL352326 | — | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL169923 | — | Kd | = | 8400.0 | nM | 5.08 |