Assay Detail
Binding
CHEMBL4682087
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Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to the depolarizing pulse by whole cell patch clamp assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Targeting of N-Type Calcium Channels via GABA-Receptor Activation by α-Conotoxin Vc1.1 Variants Displaying Improved Analgesic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.38 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763515 | — | — | 1 | 9.70 |
| CHEMBL4791366 | — | — | 1 | 8.92 |
| CHEMBL4756657 | — | — | 1 | 8.62 |
| CHEMBL4787614 | — | — | 1 | 8.31 |
| CHEMBL4745449 | — | — | 1 | 7.73 |
| CHEMBL4762233 | — | — | 1 | 7.72 |
| CHEMBL4740566 | — | — | 1 | 7.63 |
| CHEMBL4785671 | — | — | 1 | - |
| CHEMBL4780501 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763515 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4791366 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4756657 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4787614 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4745449 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL4762233 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4740566 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL4785671 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4780501 | — | IC50 | > | 1000.0 | nM | - |