Assay Detail
Binding
CHEMBL4676182
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
50
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 6.65 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4747248 | — | — | 1 | 7.75 |
| CHEMBL4537788 | BAY-784 | — | 1 | 7.68 |
| CHEMBL4741994 | — | — | 1 | 7.66 |
| CHEMBL4749974 | — | — | 2 | 7.58 |
| CHEMBL4749790 | — | — | 3 | 7.55 |
| CHEMBL4782228 | — | — | 1 | 7.46 |
| CHEMBL4762368 | — | — | 1 | 7.44 |
| CHEMBL4781434 | — | — | 2 | 7.36 |
| CHEMBL4747322 | — | — | 1 | 7.35 |
| CHEMBL4761024 | — | — | 1 | 7.33 |
| CHEMBL3358413 | — | — | 1 | 7.27 |
| CHEMBL4787856 | — | — | 1 | 7.21 |
| CHEMBL4779806 | — | — | 1 | 7.17 |
| CHEMBL4746174 | — | — | 1 | 7.11 |
| CHEMBL4780737 | — | — | 3 | 7.05 |
| CHEMBL4760799 | — | — | 1 | 7.04 |
| CHEMBL4756920 | — | — | 3 | 6.98 |
| CHEMBL4745391 | — | — | 1 | 6.88 |
| CHEMBL4740379 | — | — | 1 | 6.88 |
| CHEMBL4793643 | — | — | 1 | 6.85 |
| CHEMBL4751345 | — | — | 1 | 6.84 |
| CHEMBL4740373 | — | — | 2 | 6.76 |
| CHEMBL4757424 | — | — | 1 | 6.64 |
| CHEMBL4799511 | — | — | 1 | 6.61 |
| CHEMBL4798682 | — | — | 1 | 6.57 |
| CHEMBL4798298 | — | — | 1 | 6.51 |
| CHEMBL4746969 | — | — | 1 | 6.38 |
| CHEMBL4786609 | — | — | 1 | 6.26 |
| CHEMBL4789613 | — | — | 1 | 6.04 |
| CHEMBL4794864 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4747248 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4537788 | BAY-784 | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4741994 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4749974 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4749790 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4782228 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4762368 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4781434 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4747322 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4761024 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3358413 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4749974 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL4787856 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4779806 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4746174 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4780737 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4760799 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4749790 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4756920 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4756920 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4745391 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4740379 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4793643 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4751345 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4740373 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4740373 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4756920 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4757424 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL4799511 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4798682 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4798298 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4746969 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL4786609 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL4789613 | — | IC50 | = | 921.0 | nM | 6.04 |
| CHEMBL4794864 | — | IC50 | = | 1047.0 | nM | 5.98 |
| CHEMBL4795998 | — | IC50 | = | 1151.0 | nM | 5.94 |
| CHEMBL4787218 | — | IC50 | = | 1413.0 | nM | 5.85 |
| CHEMBL4740709 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4740709 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4782882 | — | IC50 | = | 1768.0 | nM | 5.75 |
| CHEMBL4781434 | — | IC50 | = | 2432.0 | nM | 5.61 |
| CHEMBL4740709 | — | IC50 | = | 6616.0 | nM | 5.18 |
| CHEMBL4753358 | — | IC50 | = | 13802.0 | nM | 4.86 |
| CHEMBL4752711 | — | IC50 | = | 18241.0 | nM | 4.74 |
| CHEMBL4753775 | — | IC50 | = | 18144.0 | nM | 4.74 |
| CHEMBL4780737 | — | IC50 | - | — | - | |
| CHEMBL4780737 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4749790 | — | IC50 | >= | 20.0 | 10^3nM | - |
| CHEMBL4751238 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4740709 | — | IC50 | >= | 20.0 | 10^3nM | - |