Assay Detail
Binding
CHEMBL4427195
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant P2X3 receptor expressed in HEK293-Tet-on cells assessed as alpha,beta-methylene-ATP-stimulated Ca2+ influx by Fluo-4 assay
73
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 73 | 6.41 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4476395 | — | — | 1 | 8.00 |
| CHEMBL4544380 | — | — | 1 | 7.82 |
| CHEMBL4542098 | — | — | 1 | 7.82 |
| CHEMBL4587231 | — | — | 1 | 7.82 |
| CHEMBL4439566 | — | — | 1 | 7.82 |
| CHEMBL4458821 | — | — | 1 | 7.70 |
| CHEMBL526307 | — | — | 1 | 7.70 |
| CHEMBL4448484 | — | — | 1 | 7.70 |
| CHEMBL4568965 | — | — | 1 | 7.68 |
| CHEMBL2011112 | — | — | 1 | 7.60 |
| CHEMBL4449004 | — | — | 1 | 7.60 |
| CHEMBL4546396 | — | — | 1 | 7.48 |
| CHEMBL4442508 | — | — | 1 | 7.46 |
| CHEMBL4450775 | — | — | 1 | 7.46 |
| CHEMBL4444041 | — | — | 1 | 7.40 |
| CHEMBL4440083 | — | — | 1 | 7.40 |
| CHEMBL4515308 | — | — | 1 | 7.40 |
| CHEMBL4549131 | — | — | 1 | 7.40 |
| CHEMBL3716057 | GEFAPIXANT | 4.0 | 1 | 7.35 |
| CHEMBL4547802 | — | — | 1 | 7.32 |
| CHEMBL4460871 | — | — | 1 | 7.30 |
| CHEMBL4563035 | — | — | 1 | 7.26 |
| CHEMBL4572174 | — | — | 1 | 7.19 |
| CHEMBL4440963 | — | — | 1 | 7.07 |
| CHEMBL4568398 | — | — | 1 | 6.85 |
| CHEMBL4565455 | — | — | 1 | 6.85 |
| CHEMBL4559858 | — | — | 1 | 6.82 |
| CHEMBL4451343 | — | — | 1 | 6.75 |
| CHEMBL4453198 | — | — | 1 | 6.75 |
| CHEMBL596234 | A-317491 | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4476395 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4544380 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4439566 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4542098 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4587231 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4458821 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL526307 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4448484 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4568965 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2011112 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4449004 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4546396 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4442508 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4450775 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4549131 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4440083 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4515308 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4444041 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3716057 | GEFAPIXANT | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4547802 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4460871 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4563035 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4572174 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4440963 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4565455 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4568398 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4559858 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4451343 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4453198 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL596234 | A-317491 | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4559230 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4524275 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4471519 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4454932 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4465662 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4459425 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4542643 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4463088 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4464204 | — | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL4516592 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4531994 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4589123 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4549675 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4567591 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4578016 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4439753 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4567453 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4571607 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4558507 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4448180 | — | IC50 | = | 1400.0 | nM | 5.85 |