Assay Detail
Binding
CHEMBL689137
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Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
34
Total Activities
34
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 | 34 | 8.33 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296644 | — | — | 1 | 8.70 |
| CHEMBL298074 | — | — | 1 | 8.70 |
| CHEMBL300045 | — | — | 1 | 8.70 |
| CHEMBL443768 | — | — | 1 | 8.70 |
| CHEMBL47761 | — | — | 1 | 8.70 |
| CHEMBL265774 | — | — | 1 | 8.70 |
| CHEMBL295908 | — | — | 1 | 8.70 |
| CHEMBL42592 | — | — | 1 | 8.70 |
| CHEMBL300268 | — | — | 1 | 8.70 |
| CHEMBL295152 | — | — | 1 | 8.52 |
| CHEMBL49542 | — | — | 1 | 8.52 |
| CHEMBL46268 | — | — | 1 | 8.52 |
| CHEMBL48763 | — | — | 1 | 8.52 |
| CHEMBL49891 | — | — | 1 | 8.52 |
| CHEMBL239108 | — | — | 1 | 8.52 |
| CHEMBL297918 | — | — | 1 | 8.52 |
| CHEMBL297927 | — | — | 1 | 8.52 |
| CHEMBL49578 | — | — | 1 | 8.52 |
| CHEMBL45489 | — | — | 1 | 8.52 |
| CHEMBL47862 | — | — | 1 | 8.40 |
| CHEMBL445848 | — | — | 1 | 8.40 |
| CHEMBL298748 | — | — | 1 | 8.40 |
| CHEMBL291201 | — | — | 1 | 8.40 |
| CHEMBL49893 | — | — | 1 | 8.30 |
| CHEMBL297430 | — | — | 1 | 8.30 |
| CHEMBL295731 | — | — | 1 | 8.30 |
| CHEMBL45639 | — | — | 1 | 8.22 |
| CHEMBL416285 | — | — | 1 | 8.22 |
| CHEMBL11149 | — | — | 1 | 8.15 |
| CHEMBL47227 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296644 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL298074 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL300045 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL443768 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL47761 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL265774 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL295908 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL42592 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL300268 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL46268 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL49542 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL48763 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL295152 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL49891 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL297918 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL297927 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL49578 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL45489 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL239108 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL47862 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL445848 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL298748 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL291201 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL297430 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL295731 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL49893 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL45639 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL416285 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL11149 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL47227 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL416286 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL46385 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL10931 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL47921 | — | IC50 | = | 600.0 | nM | 6.22 |