Assay Detail
Binding
CHEMBL4430592
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
80
Total Activities
80
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 80 | 6.72 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593521 | — | — | 1 | 8.27 |
| CHEMBL4463476 | — | — | 1 | 7.90 |
| CHEMBL4449332 | — | — | 1 | 7.89 |
| CHEMBL4474379 | — | — | 1 | 7.78 |
| CHEMBL4460880 | — | — | 1 | 7.63 |
| CHEMBL4585638 | — | — | 1 | 7.57 |
| CHEMBL4582367 | — | — | 1 | 7.56 |
| CHEMBL4544693 | — | — | 1 | 7.55 |
| CHEMBL4575491 | — | — | 1 | 7.38 |
| CHEMBL4540232 | — | — | 1 | 7.30 |
| CHEMBL4567854 | — | — | 1 | 7.29 |
| CHEMBL4452636 | — | — | 1 | 7.28 |
| CHEMBL4467407 | — | — | 1 | 7.22 |
| CHEMBL4536130 | — | — | 1 | 7.21 |
| CHEMBL4521484 | — | — | 1 | 7.21 |
| CHEMBL4539811 | — | — | 1 | 7.19 |
| CHEMBL4456937 | — | — | 1 | 7.06 |
| CHEMBL179691 | — | — | 1 | 7.06 |
| CHEMBL4566719 | — | — | 1 | 7.05 |
| CHEMBL4436854 | — | — | 1 | 6.99 |
| CHEMBL4516712 | — | — | 1 | 6.99 |
| CHEMBL4520639 | — | — | 1 | 6.97 |
| CHEMBL4439926 | — | — | 1 | 6.94 |
| CHEMBL4563686 | — | — | 1 | 6.91 |
| CHEMBL4461692 | — | — | 1 | 6.84 |
| CHEMBL4473168 | — | — | 1 | 6.77 |
| CHEMBL4449450 | — | — | 1 | 6.75 |
| CHEMBL4590493 | — | — | 1 | 6.74 |
| CHEMBL4456703 | — | — | 1 | 6.71 |
| CHEMBL4443108 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593521 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4463476 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4449332 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4474379 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL4460880 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL4585638 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL4582367 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL4544693 | — | IC50 | = | 27.9 | nM | 7.55 |
| CHEMBL4575491 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4540232 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL4567854 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL4452636 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4467407 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4521484 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4536130 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4539811 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4456937 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL179691 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4566719 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL4436854 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4516712 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4520639 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4439926 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4563686 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4461692 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4473168 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4449450 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4590493 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL4456703 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4443108 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4474058 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL4473194 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL4476330 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4446131 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4526641 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL4583933 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4557575 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4464132 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4576169 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4447139 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL4522657 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL4173938 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL4550720 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL4567165 | — | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL4472942 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL4517137 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL4446435 | — | IC50 | = | 885.0 | nM | 6.05 |
| CHEMBL4439817 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4526188 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4436711 | — | IC50 | = | 1180.0 | nM | 5.93 |