Assay Detail
Binding
CHEMBL5734856
Review assay metadata, readout intent, target linkage, and publication context from the same page.
3H-SB222200 Binding Competition Assay with Human NK-3 Receptor: The ability of the compounds of the invention to inhibit the binding of the NK-3 receptor selective antagonist SB222200 was assessed by an in vitro radioligand binding assay. Membranes were prepared from Chinese hamster ovary recombinant cells which express the human NK3 receptor. The membranes were incubated with 5 nM 3H-SB222200_(ARC) in a HEPES 25 mM/NaCl 0.1M/CaCl2 1 mM/MgCl2 5 Mm/BSA 0.5%/Saponin 10 μg/ml buffer at pH 7.4 and various concentrations of the compounds of the invention. The amount of tritiated SB222200 bound to the receptor was determined after filtration by the quantification of membrane associated radioactivity using the TopCount-NXT reader (Packard). Competition curves were obtained for compounds of the invention and the concentrations of compounds which displaced 50% of bound radioligand (IC50) were determined and then apparent inhibition constant Ki values were calculated by the following equation: Ki=IC50/(1+[L]/KD) where [L] is the concentration of free radioligand and KD is its dissociation constant at the receptor, derived from saturation binding experiments (Cheng and Prusoff, 1973).
669
Total Activities
221
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 223 | 5.77 | 6.12 |
| kon | 223 | - | - |
| k_off | 223 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5891680 | — | — | 3 | 6.12 |
| CHEMBL5783937 | — | — | 3 | 6.12 |
| CHEMBL5968656 | — | — | 3 | 6.12 |
| CHEMBL5926040 | — | — | 3 | 6.12 |
| CHEMBL5821915 | — | — | 3 | 6.12 |
| CHEMBL5767259 | — | — | 3 | 6.12 |
| CHEMBL5781721 | — | — | 3 | 6.12 |
| CHEMBL5755444 | — | — | 3 | 6.12 |
| CHEMBL5928565 | — | — | 3 | 6.12 |
| CHEMBL5876732 | — | — | 3 | 6.12 |
| CHEMBL6001927 | — | — | 3 | 6.12 |
| CHEMBL5871289 | — | — | 3 | 6.12 |
| CHEMBL5798092 | — | — | 3 | 6.12 |
| CHEMBL5811722 | — | — | 3 | 6.12 |
| CHEMBL5759489 | — | — | 3 | 6.12 |
| CHEMBL3422004 | — | — | 3 | 6.12 |
| CHEMBL5833907 | — | — | 3 | 6.12 |
| CHEMBL6016002 | — | — | 3 | 6.12 |
| CHEMBL5807413 | — | — | 3 | 6.12 |
| CHEMBL5826717 | — | — | 3 | 6.12 |
| CHEMBL5878886 | — | — | 3 | 6.12 |
| CHEMBL5852480 | — | — | 3 | 6.12 |
| CHEMBL5783714 | — | — | 3 | 6.12 |
| CHEMBL6048322 | — | — | 3 | 6.12 |
| CHEMBL5796446 | — | — | 3 | 6.12 |
| CHEMBL3421983 | — | — | 3 | 5.52 |
| CHEMBL5742377 | — | — | 3 | 5.52 |
| CHEMBL3421996 | — | — | 3 | 5.52 |
| CHEMBL5918503 | — | — | 3 | 5.52 |
| CHEMBL5786801 | — | — | 3 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5755444 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5928565 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5826717 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5833907 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5926040 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5807413 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5811722 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5783714 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5767259 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5968656 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL6016002 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5783937 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5759489 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL6048322 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5878886 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5871289 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL3422004 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL6001927 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5852480 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5781721 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5876732 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5821915 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5796446 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5891680 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5798092 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL6049599 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5956283 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL6051223 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5798451 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5908967 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3421983 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5804129 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5918503 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5926961 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5941688 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5786801 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5795472 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3421990 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL6013086 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5990807 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5815668 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3421998 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL6014616 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5772148 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5988379 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5951092 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5945182 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5816352 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL6028714 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL6024430 | — | Ki | = | 3000.0 | nM | 5.52 |