Assay Detail
Functional
CHEMBL710602
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Inhibition of phosphoinositol hydrolysis of MMQ cells.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MMQ |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Expert |
Publication
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.71 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 10.40 |
| CHEMBL8923 | — | — | 1 | 9.80 |
| CHEMBL9139 | — | — | 1 | 9.62 |
| CHEMBL9334 | — | — | 1 | 9.60 |
| CHEMBL9119 | — | — | 1 | 9.55 |
| CHEMBL9502 | — | — | 1 | 9.48 |
| CHEMBL266354 | — | — | 1 | 9.22 |
| CHEMBL267695 | — | — | 1 | 9.01 |
| CHEMBL267279 | — | — | 1 | 9.00 |
| CHEMBL9488 | — | — | 1 | 8.87 |
| CHEMBL8736 | — | — | 1 | 8.69 |
| CHEMBL9212 | — | — | 1 | 8.65 |
| CHEMBL9223 | — | — | 1 | 8.31 |
| CHEMBL9050 | — | — | 1 | 8.25 |
| CHEMBL266594 | — | — | 1 | 8.04 |
| CHEMBL266337 | — | — | 1 | 8.04 |
| CHEMBL267761 | — | — | 1 | 8.00 |
| CHEMBL9342 | — | — | 1 | 7.78 |
| CHEMBL268864 | — | — | 1 | 7.62 |
| CHEMBL9141 | — | — | 1 | 7.61 |
| CHEMBL428504 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL8923 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL9139 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL9334 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL9119 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL9502 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL266354 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL267695 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL267279 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL9488 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL8736 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL9212 | — | IC50 | = | 2.26 | nM | 8.65 |
| CHEMBL9223 | — | IC50 | = | 4.91 | nM | 8.31 |
| CHEMBL9050 | — | IC50 | = | 5.64 | nM | 8.25 |
| CHEMBL266594 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL266337 | — | IC50 | = | 9.22 | nM | 8.04 |
| CHEMBL267761 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL9342 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL268864 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL9141 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL428504 | — | IC50 | = | 46.8 | nM | 7.33 |