Assay Detail
Binding
CHEMBL5375221
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Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.43 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410506 | — | — | 1 | 6.05 |
| CHEMBL5405597 | — | — | 1 | 5.47 |
| CHEMBL5423734 | — | — | 1 | 5.35 |
| CHEMBL5398023 | — | — | 1 | 5.35 |
| CHEMBL5394725 | — | — | 1 | 4.95 |
| CHEMBL5414539 | — | — | 1 | - |
| CHEMBL5420748 | — | — | 1 | - |
| CHEMBL5401699 | — | — | 1 | - |
| CHEMBL5427163 | — | — | 1 | - |
| CHEMBL5396623 | — | — | 1 | - |
| CHEMBL5421688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410506 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL5405597 | — | EC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL5423734 | — | EC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL5398023 | — | EC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL5394725 | — | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL5414539 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5420748 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5401699 | — | EC50 | > | 31622.78 | nM | - |
| CHEMBL5427163 | — | EC50 | > | 31622.78 | nM | - |
| CHEMBL5396623 | — | EC50 | > | 31622.78 | nM | - |
| CHEMBL5421688 | — | EC50 | > | 31622.78 | nM | - |