Assay Detail
Binding
CHEMBL1006036
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Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.54 | 6.20 |
| Ki | 6 | 6.22 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499519 | NOCARDIMICIN B | — | 2 | 6.89 |
| CHEMBL450986 | NOCARDIMICIN D | — | 2 | 6.64 |
| CHEMBL510340 | NOCCARDIMICIN E | — | 2 | 6.01 |
| CHEMBL507760 | NOCARDIMICIN C | — | 2 | 6.00 |
| CHEMBL505197 | NOCARDIMICIN A | — | 2 | 5.90 |
| CHEMBL508807 | NOCARDIMICIN F | — | 2 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499519 | NOCARDIMICIN B | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL450986 | NOCARDIMICIN D | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL499519 | NOCARDIMICIN B | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL510340 | NOCCARDIMICIN E | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL507760 | NOCARDIMICIN C | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL450986 | NOCARDIMICIN D | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL505197 | NOCARDIMICIN A | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL508807 | NOCARDIMICIN F | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL510340 | NOCCARDIMICIN E | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL507760 | NOCARDIMICIN C | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL505197 | NOCARDIMICIN A | IC50 | = | 5890.0 | nM | 5.23 |
| CHEMBL508807 | NOCARDIMICIN F | IC50 | = | 6290.0 | nM | 5.20 |