Assay Detail
Functional
CHEMBL3721001
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against rat P2X3 receptor expressed in CHOK1 cells assessed as inhibition of alpha,beta-meATP-induced calcium response incubated for 20 mins by Fluo-3AM dye based FLIPR assay
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.91 | 8.66 |
| IC50 | 1 | 8.24 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3715500 | — | — | 1 | 8.66 |
| CHEMBL494161 | — | — | 1 | 8.53 |
| CHEMBL3717153 | — | — | 1 | 8.24 |
| CHEMBL523173 | — | — | 1 | 8.24 |
| CHEMBL495204 | — | — | 1 | 8.20 |
| CHEMBL494353 | — | — | 1 | 8.15 |
| CHEMBL494160 | — | — | 1 | 8.12 |
| CHEMBL3718402 | — | — | 1 | 8.08 |
| CHEMBL3715231 | — | — | 1 | 8.02 |
| CHEMBL526307 | — | — | 1 | 8.01 |
| CHEMBL492300 | — | — | 1 | 8.00 |
| CHEMBL2304566 | — | — | 1 | 7.99 |
| CHEMBL3715486 | — | — | 1 | 7.98 |
| CHEMBL3718862 | — | — | 1 | 7.95 |
| CHEMBL3716526 | — | — | 1 | 7.94 |
| CHEMBL494159 | — | — | 1 | 7.93 |
| CHEMBL492907 | — | — | 1 | 7.84 |
| CHEMBL3718425 | — | — | 1 | 7.77 |
| CHEMBL3716384 | — | — | 1 | 7.44 |
| CHEMBL3716057 | GEFAPIXANT | 4.0 | 1 | 7.15 |
| CHEMBL3717944 | — | — | 1 | 7.11 |
| CHEMBL494581 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3715500 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL494161 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL3717153 | — | IC50 | = | 5.754 | nM | 8.24 |
| CHEMBL523173 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL495204 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL494353 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL494160 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL3718402 | — | Ki | = | 8.318 | nM | 8.08 |
| CHEMBL3715231 | — | Ki | = | 9.55 | nM | 8.02 |
| CHEMBL526307 | — | Ki | = | 9.772 | nM | 8.01 |
| CHEMBL492300 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2304566 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL3715486 | — | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL3718862 | — | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL3716526 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL494159 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL492907 | — | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL3718425 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL3716384 | — | Ki | = | 36.31 | nM | 7.44 |
| CHEMBL3716057 | GEFAPIXANT | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL3717944 | — | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL494581 | — | Ki | = | 102.33 | nM | 6.99 |