Assay Detail
Binding
CHEMBL4381891
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Inhibition of human P2X3 assessed as reduction in agonist-induced intracellular Ca2+ concentration pre-incubated for 30 mins before agonist addition by calcium 5 dye based fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.35 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL241106 | ARCHAZOLID A | — | 1 | 7.07 |
| CHEMBL411767 | ARCHAZOLID B | — | 1 | 6.45 |
| CHEMBL1784269 | ARCHAZOLID F | — | 1 | 6.36 |
| CHEMBL4593430 | — | — | 1 | 6.19 |
| CHEMBL290814 | BAFILOMYCIN A1 | — | 1 | 6.12 |
| CHEMBL4471610 | — | — | 1 | 5.88 |
| CHEMBL4549217 | — | — | 1 | - |
| CHEMBL4447903 | — | — | 1 | - |
| CHEMBL4460252 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL241106 | ARCHAZOLID A | IC50 | = | 86.1 | nM | 7.07 |
| CHEMBL411767 | ARCHAZOLID B | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL1784269 | ARCHAZOLID F | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL4593430 | — | IC50 | = | 648.0 | nM | 6.19 |
| CHEMBL290814 | BAFILOMYCIN A1 | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL4471610 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4549217 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4447903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4460252 | — | IC50 | > | 2000.0 | nM | - |