Assay Detail
Functional
CHEMBL4263113
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.64 | 8.30 |
| Ki | 13 | 7.35 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71917 | — | — | 2 | 10.00 |
| CHEMBL515123 | — | — | 2 | 7.91 |
| CHEMBL4283577 | — | — | 2 | 7.86 |
| CHEMBL494803 | — | — | 2 | 7.72 |
| CHEMBL4282476 | — | — | 2 | 7.42 |
| CHEMBL4285058 | — | — | 2 | 6.98 |
| CHEMBL4286937 | — | — | 2 | 6.80 |
| CHEMBL4294163 | — | — | 2 | 6.73 |
| CHEMBL4280124 | — | — | 2 | 6.59 |
| CHEMBL4290761 | — | — | 2 | 6.40 |
| CHEMBL4277116 | — | — | 2 | 6.39 |
| CHEMBL4279003 | — | — | 2 | - |
| CHEMBL4290349 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71917 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL71917 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL515123 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL4283577 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL494803 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4282476 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4285058 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL4286937 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4294163 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL4280124 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL4290761 | — | Ki | = | 395.0 | nM | 6.40 |
| CHEMBL4277116 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL515123 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4283577 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL494803 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4282476 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4285058 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4286937 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4294163 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4280124 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4290761 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4277116 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4279003 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4290349 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4290349 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4279003 | — | IC50 | > | 10000.0 | nM | - |