Assay Detail
Binding
CHEMBL677091
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.24 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL263079 | — | — | 1 | 8.60 |
| CHEMBL268174 | — | — | 1 | 8.10 |
| CHEMBL6412 | — | — | 1 | 8.00 |
| CHEMBL6555 | — | — | 1 | 7.80 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.30 |
| CHEMBL6800 | — | — | 1 | 7.20 |
| CHEMBL268339 | — | — | 1 | 6.90 |
| CHEMBL6553 | — | — | 1 | 6.80 |
| CHEMBL6761 | — | — | 1 | 6.70 |
| CHEMBL6297 | — | — | 1 | 6.60 |
| CHEMBL266277 | — | — | 1 | 6.60 |
| CHEMBL6624 | — | — | 1 | 6.50 |
| CHEMBL268116 | — | — | 1 | 6.50 |
| CHEMBL415106 | — | — | 1 | 6.40 |
| CHEMBL6588 | — | — | 1 | 6.30 |
| CHEMBL7019 | — | — | 1 | 6.20 |
| CHEMBL6382 | — | — | 1 | 6.20 |
| CHEMBL6399 | — | — | 1 | 6.00 |
| CHEMBL6583 | — | — | 1 | 5.90 |
| CHEMBL415292 | — | — | 1 | 5.90 |
| CHEMBL6433 | — | — | 1 | 5.80 |
| CHEMBL6411 | — | — | 1 | 5.80 |
| CHEMBL268387 | — | — | 1 | 5.80 |
| CHEMBL6463 | — | — | 1 | 5.80 |
| CHEMBL6576 | — | — | 1 | 5.70 |
| CHEMBL6630 | — | — | 1 | 5.70 |
| CHEMBL266315 | — | — | 1 | 5.70 |
| CHEMBL6543 | — | — | 1 | 5.60 |
| CHEMBL6400 | — | — | 1 | 5.50 |
| CHEMBL269237 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL263079 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL268174 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL6412 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6555 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL267458 | BMS-182874 | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL6800 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL268339 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL6553 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL6761 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL266277 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL6297 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL6624 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL268116 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL415106 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL6588 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL7019 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL6382 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL6399 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL6583 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL415292 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL6433 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL6411 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL268387 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL6463 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL6576 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL6630 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL266315 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL6543 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL6400 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL269237 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL6660 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL266684 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL6647 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL6468 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL6778 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL6566 | — | IC50 | = | 10000.0 | nM | 5.00 |