Assay Detail
Binding
CHEMBL745740
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Binding affinity against M1 receptor expressed in CHO-K1 cells transfected with human muscarinic receptor sequence using radioligand [3H]quinuclidinyl benzilate ([3H]QNB)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 6.31 | 6.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277642 | HIMBACINE | — | 1 | 6.83 |
| CHEMBL160666 | — | — | 1 | 6.78 |
| CHEMBL159237 | — | — | 1 | 6.37 |
| CHEMBL346049 | — | — | 1 | 6.31 |
| CHEMBL159189 | — | — | 1 | 6.22 |
| CHEMBL160755 | — | — | 1 | 6.06 |
| CHEMBL158589 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277642 | HIMBACINE | Kd | = | 148.0 | nM | 6.83 |
| CHEMBL160666 | — | Kd | = | 167.0 | nM | 6.78 |
| CHEMBL159237 | — | Kd | = | 423.0 | nM | 6.37 |
| CHEMBL346049 | — | Kd | = | 494.0 | nM | 6.31 |
| CHEMBL159189 | — | Kd | = | 604.7 | nM | 6.22 |
| CHEMBL160755 | — | Kd | = | 866.0 | nM | 6.06 |
| CHEMBL158589 | — | Kd | = | 2520.0 | nM | 5.60 |