Assay Detail
Binding
CHEMBL954319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.62 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460480 | — | — | 1 | 8.77 |
| CHEMBL521674 | — | — | 1 | 8.15 |
| CHEMBL494400 | — | — | 1 | 8.12 |
| CHEMBL493731 | — | — | 1 | 8.10 |
| CHEMBL523711 | — | — | 1 | 8.00 |
| CHEMBL492327 | — | — | 1 | 8.00 |
| CHEMBL493730 | — | — | 1 | 7.96 |
| CHEMBL493167 | — | — | 1 | 7.92 |
| CHEMBL493344 | — | — | 1 | 7.75 |
| CHEMBL494738 | — | — | 1 | 7.75 |
| CHEMBL523849 | — | — | 1 | 7.72 |
| CHEMBL523527 | — | — | 1 | 7.70 |
| CHEMBL494554 | — | — | 1 | 7.68 |
| CHEMBL495174 | — | — | 1 | 7.68 |
| CHEMBL495183 | — | — | 1 | 7.66 |
| CHEMBL522202 | — | — | 1 | 7.64 |
| CHEMBL494739 | — | — | 1 | 7.58 |
| CHEMBL494416 | — | — | 1 | 7.57 |
| CHEMBL522188 | — | — | 1 | 7.57 |
| CHEMBL493931 | — | — | 1 | 7.54 |
| CHEMBL494232 | — | — | 1 | 7.51 |
| CHEMBL492780 | — | — | 1 | 7.48 |
| CHEMBL494415 | — | — | 1 | 7.43 |
| CHEMBL495190 | — | — | 1 | 7.42 |
| CHEMBL493185 | — | — | 1 | 7.37 |
| CHEMBL493565 | — | — | 1 | 7.34 |
| CHEMBL493932 | — | — | 1 | 7.24 |
| CHEMBL495189 | — | — | 1 | 7.17 |
| CHEMBL494021 | — | — | 1 | 7.08 |
| CHEMBL492587 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460480 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL521674 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL494400 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL493731 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL523711 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL492327 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL493730 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL493167 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL493344 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL494738 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL523849 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL523527 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL494554 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL495174 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL495183 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL522202 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL494739 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL494416 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL522188 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL493931 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL494232 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL492780 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL494415 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL495190 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL493185 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL493565 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL493932 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL495189 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL494021 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL492587 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL494548 | — | IC50 | = | 705.0 | nM | 6.15 |