Assay Detail
Functional
CHEMBL1035691
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Antagonist activity at cloned muscarinic M2 receptor-Gqi5 chimeric protein expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 7.42 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521523 | — | — | 1 | 8.30 |
| CHEMBL555476 | — | — | 1 | 7.90 |
| CHEMBL493266 | — | — | 1 | 7.60 |
| CHEMBL492437 | — | — | 1 | 7.20 |
| CHEMBL493265 | — | — | 1 | 7.00 |
| CHEMBL493465 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521523 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL555476 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL493266 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL492437 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL493265 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL493465 | — | Kd | = | 316.23 | nM | 6.50 |