Assay Detail
Binding
CHEMBL898460
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
60
Total Activities
60
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 59 | 6.69 | 8.30 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392605 | — | — | 1 | 8.30 |
| CHEMBL235270 | — | — | 1 | 8.30 |
| CHEMBL236152 | — | — | 1 | 8.00 |
| CHEMBL413238 | — | — | 1 | 8.00 |
| CHEMBL235269 | — | — | 1 | 8.00 |
| CHEMBL262579 | — | — | 1 | 7.82 |
| CHEMBL16745 | — | — | 1 | 7.82 |
| CHEMBL236127 | — | — | 1 | 7.77 |
| CHEMBL393092 | — | — | 1 | 7.70 |
| CHEMBL242399 | — | — | 1 | 7.70 |
| CHEMBL392731 | — | — | 1 | 7.60 |
| CHEMBL236142 | — | — | 1 | 7.52 |
| CHEMBL392602 | — | — | 1 | 7.52 |
| CHEMBL235520 | — | — | 1 | 7.46 |
| CHEMBL392709 | — | — | 1 | 7.35 |
| CHEMBL430171 | — | — | 1 | 7.16 |
| CHEMBL262581 | — | — | 1 | 7.10 |
| CHEMBL236332 | — | — | 1 | 7.07 |
| CHEMBL235051 | — | — | 1 | 7.00 |
| CHEMBL236966 | — | — | 1 | 6.80 |
| CHEMBL236342 | — | — | 1 | 6.75 |
| CHEMBL392604 | — | — | 1 | 6.59 |
| CHEMBL392607 | — | — | 1 | 6.52 |
| CHEMBL235050 | — | — | 1 | 6.52 |
| CHEMBL262580 | — | — | 1 | 6.42 |
| CHEMBL236967 | — | — | 1 | 6.31 |
| CHEMBL236546 | — | — | 1 | 6.29 |
| CHEMBL392815 | — | — | 1 | 6.28 |
| CHEMBL395183 | — | — | 1 | 6.27 |
| CHEMBL235046 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392605 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL235270 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL413238 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL235269 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL236152 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL262579 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL16745 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL236127 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL393092 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL242399 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL392731 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL236142 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL392602 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL235520 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL392709 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL430171 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL262581 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL236332 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL235051 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL236966 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL236342 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL392604 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL392607 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL235050 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL262580 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL236967 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL236546 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL392815 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL395183 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL235046 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL392603 | — | Ki | = | 805.0 | nM | 6.09 |
| CHEMBL236331 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL413239 | — | Ki | = | 945.0 | nM | 6.03 |
| CHEMBL398583 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL236545 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL235084 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL236544 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL235519 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL393093 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL392688 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL236750 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL392087 | — | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL236137 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL412581 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL236197 | — | Ki | = | 2410.0 | nM | 5.62 |
| CHEMBL236550 | — | Ki | = | 2450.0 | nM | 5.61 |
| CHEMBL392733 | — | Ki | = | 2590.0 | nM | 5.59 |
| CHEMBL236965 | — | Ki | = | 2580.0 | nM | 5.59 |
| CHEMBL237640 | — | Activity | - | — | - | |
| CHEMBL236751 | — | Ki | > | 10000.0 | nM | - |