Assay Detail
Binding
CHEMBL689138
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 9.56 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298074 | — | — | 1 | 10.00 |
| CHEMBL49891 | — | — | 1 | 10.00 |
| CHEMBL297918 | — | — | 1 | 10.00 |
| CHEMBL45597 | — | — | 1 | 9.92 |
| CHEMBL49542 | — | — | 1 | 9.70 |
| CHEMBL239108 | — | — | 1 | 9.70 |
| CHEMBL47862 | — | — | 1 | 9.70 |
| CHEMBL295152 | — | — | 1 | 9.70 |
| CHEMBL265774 | — | — | 1 | 9.70 |
| CHEMBL42592 | — | — | 1 | 9.70 |
| CHEMBL443768 | — | — | 1 | 9.70 |
| CHEMBL300045 | — | — | 1 | 9.70 |
| CHEMBL47761 | — | — | 1 | 9.70 |
| CHEMBL45489 | — | — | 1 | 9.52 |
| CHEMBL297927 | — | — | 1 | 9.52 |
| CHEMBL297430 | — | — | 1 | 9.40 |
| CHEMBL297151 | — | — | 1 | 9.40 |
| CHEMBL49578 | — | — | 1 | 9.40 |
| CHEMBL298748 | — | — | 1 | 9.30 |
| CHEMBL416285 | — | — | 1 | 9.30 |
| CHEMBL48069 | — | — | 1 | 9.10 |
| CHEMBL45614 | — | — | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298074 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL49891 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL297918 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL45597 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL49542 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL239108 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL47862 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL295152 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL265774 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL42592 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL443768 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL300045 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL47761 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL45489 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL297927 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL297430 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL297151 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL49578 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL298748 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL416285 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL48069 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL45614 | — | IC50 | = | 5.7 | nM | 8.24 |