Assay Detail
Binding
CHEMBL680259
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Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Pituitary gland |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Betidamino acid scan of the GnRH antagonist acyline.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 8.67 | 10.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268095 | — | — | 1 | 10.25 |
| CHEMBL216519 | — | — | 1 | 9.64 |
| CHEMBL415351 | — | — | 1 | 9.52 |
| CHEMBL407316 | — | — | 1 | 9.52 |
| CHEMBL412472 | — | — | 1 | 9.52 |
| CHEMBL262825 | — | — | 1 | 9.52 |
| CHEMBL413752 | — | — | 1 | 9.42 |
| CHEMBL407681 | — | — | 1 | 9.37 |
| CHEMBL2370593 | — | — | 1 | 9.32 |
| CHEMBL2370590 | — | — | 1 | 9.30 |
| CHEMBL263358 | — | — | 1 | 9.29 |
| CHEMBL2370592 | — | — | 1 | 9.28 |
| CHEMBL407615 | — | — | 1 | 9.23 |
| CHEMBL267642 | — | — | 1 | 9.21 |
| CHEMBL262842 | — | — | 1 | 9.20 |
| CHEMBL407058 | — | — | 1 | 9.20 |
| CHEMBL414558 | — | — | 1 | 9.19 |
| CHEMBL2370594 | — | — | 1 | 9.17 |
| CHEMBL414469 | — | — | 1 | 9.13 |
| CHEMBL414468 | — | — | 1 | 9.12 |
| CHEMBL410798 | — | — | 1 | 9.08 |
| CHEMBL436683 | — | — | 1 | 9.06 |
| CHEMBL262309 | — | — | 1 | 9.05 |
| CHEMBL2370589 | — | — | 1 | 9.05 |
| CHEMBL429902 | — | — | 1 | 8.92 |
| CHEMBL436897 | — | — | 1 | 8.85 |
| CHEMBL405736 | — | — | 1 | 8.77 |
| CHEMBL410818 | — | — | 1 | 8.72 |
| CHEMBL410799 | — | — | 1 | 8.70 |
| CHEMBL269097 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268095 | — | IC50 | = | 0.056 | nM | 10.25 |
| CHEMBL216519 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL407316 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL412472 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL262825 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL415351 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL413752 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL407681 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL2370593 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL2370590 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL263358 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2370592 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL407615 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL267642 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL407058 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL262842 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL414558 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL2370594 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL414469 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL414468 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL410798 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL436683 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL2370589 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL262309 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL429902 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL436897 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL405736 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL410818 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL410799 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL269097 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL411144 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL413456 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL444903 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL408335 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL263629 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL265727 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL407193 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL439258 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL216112 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL429381 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL384385 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL263200 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL406211 | — | IC50 | > | 1000.0 | nM | - |