Assay Detail
Binding
CHEMBL709249
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.38 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435167 | — | — | 1 | 10.00 |
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 10.00 |
| CHEMBL2092994 | — | — | 1 | 10.00 |
| CHEMBL20511 | — | — | 1 | 9.70 |
| CHEMBL21217 | — | — | 1 | 9.70 |
| CHEMBL544440 | — | — | 1 | 9.70 |
| CHEMBL280126 | — | — | 1 | 9.70 |
| CHEMBL280365 | — | — | 1 | 9.52 |
| CHEMBL21126 | — | — | 1 | 9.52 |
| CHEMBL277214 | — | — | 1 | 9.40 |
| CHEMBL280213 | — | — | 1 | 9.40 |
| CHEMBL21936 | — | — | 1 | 9.22 |
| CHEMBL280170 | — | — | 1 | 9.00 |
| CHEMBL280212 | — | — | 1 | 9.00 |
| CHEMBL21185 | — | — | 1 | 7.70 |
| CHEMBL282679 | — | — | 1 | 7.70 |
| CHEMBL279223 | — | — | 1 | 7.70 |
| CHEMBL280350 | — | — | 1 | 7.52 |
| CHEMBL21373 | — | — | 1 | 7.30 |
| CHEMBL277435 | — | — | 1 | 7.10 |
| CHEMBL281167 | — | — | 1 | 6.70 |
| CHEMBL277653 | — | — | 1 | 6.70 |
| CHEMBL277436 | — | — | 1 | 6.70 |
| CHEMBL21804 | — | — | 1 | 6.40 |
| CHEMBL21704 | — | — | 1 | 6.40 |
| CHEMBL436346 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435167 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL2092994 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL20511 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL21217 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL544440 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL280126 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL280365 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL21126 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL277214 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL280213 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL21936 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL280170 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL280212 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL21185 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL282679 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL279223 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL280350 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL21373 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL277435 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL281167 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL277653 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL277436 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL21804 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL21704 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL436346 | — | IC50 | = | 700.0 | nM | 6.16 |