Assay Detail
Functional
CHEMBL5347180
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Antagonist activity at human GnRH-R expressed in HEK293 cells assessed as changes in intracellular cytosolic Ca2+ concentration by Fluo-4 Direct based FLIPR analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.32 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800157 | — | — | 1 | 9.17 |
| CHEMBL5403996 | — | — | 1 | 9.02 |
| CHEMBL5395542 | — | — | 1 | 8.95 |
| CHEMBL5427278 | — | — | 1 | 8.79 |
| CHEMBL5434324 | — | — | 1 | 8.77 |
| CHEMBL5419489 | — | — | 1 | 8.75 |
| CHEMBL5425604 | — | — | 1 | 8.73 |
| CHEMBL5413078 | — | — | 1 | 8.69 |
| CHEMBL5432553 | — | — | 1 | 8.69 |
| CHEMBL5400302 | — | — | 1 | 8.68 |
| CHEMBL5420128 | — | — | 1 | 8.66 |
| CHEMBL5398152 | — | — | 1 | 8.64 |
| CHEMBL5419365 | — | — | 1 | 8.63 |
| CHEMBL5433025 | — | — | 1 | 8.54 |
| CHEMBL1800159 | RELUGOLIX | 4.0 | 1 | 8.39 |
| CHEMBL5414381 | — | — | 1 | 8.38 |
| CHEMBL5409192 | — | — | 1 | 8.33 |
| CHEMBL5424526 | — | — | 1 | 8.19 |
| CHEMBL5422863 | — | — | 1 | 7.96 |
| CHEMBL5404509 | — | — | 1 | 7.88 |
| CHEMBL5429424 | — | — | 1 | 7.51 |
| CHEMBL5441000 | — | — | 1 | 7.20 |
| CHEMBL5416399 | — | — | 1 | 7.05 |
| CHEMBL5407004 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800157 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5403996 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL5395542 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL5427278 | — | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL5434324 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5419489 | — | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL5425604 | — | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL5413078 | — | IC50 | = | 2.03 | nM | 8.69 |
| CHEMBL5432553 | — | IC50 | = | 2.03 | nM | 8.69 |
| CHEMBL5400302 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL5420128 | — | IC50 | = | 2.18 | nM | 8.66 |
| CHEMBL5398152 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL5419365 | — | IC50 | = | 2.34 | nM | 8.63 |
| CHEMBL5433025 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL1800159 | RELUGOLIX | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL5414381 | — | IC50 | = | 4.17 | nM | 8.38 |
| CHEMBL5409192 | — | IC50 | = | 4.71 | nM | 8.33 |
| CHEMBL5424526 | — | IC50 | = | 6.46 | nM | 8.19 |
| CHEMBL5422863 | — | IC50 | = | 10.94 | nM | 7.96 |
| CHEMBL5404509 | — | IC50 | = | 13.33 | nM | 7.88 |
| CHEMBL5429424 | — | IC50 | = | 31.14 | nM | 7.51 |
| CHEMBL5441000 | — | IC50 | = | 63.35 | nM | 7.20 |
| CHEMBL5416399 | — | IC50 | = | 88.51 | nM | 7.05 |
| CHEMBL5407004 | — | IC50 | = | 671.62 | nM | 6.17 |