Assay Detail
Functional
CHEMBL3721002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human P2X2/3 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 | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
P2X2/P2X3 heterotrimeric receptor (CHEMBL3831281) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.48 | 8.42 |
| IC50 | 1 | 7.99 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3715500 | — | — | 1 | 8.42 |
| CHEMBL494161 | — | — | 1 | 8.10 |
| CHEMBL3717153 | — | — | 1 | 7.99 |
| CHEMBL495204 | — | — | 1 | 7.94 |
| CHEMBL3718862 | — | — | 1 | 7.81 |
| CHEMBL523173 | — | — | 1 | 7.81 |
| CHEMBL3718402 | — | — | 1 | 7.79 |
| CHEMBL492300 | — | — | 1 | 7.78 |
| CHEMBL3716526 | — | — | 1 | 7.61 |
| CHEMBL3715486 | — | — | 1 | 7.60 |
| CHEMBL494159 | — | — | 1 | 7.57 |
| CHEMBL2304566 | — | — | 1 | 7.52 |
| CHEMBL494160 | — | — | 1 | 7.51 |
| CHEMBL494353 | — | — | 1 | 7.45 |
| CHEMBL526307 | — | — | 1 | 7.38 |
| CHEMBL3715231 | — | — | 1 | 7.30 |
| CHEMBL492907 | — | — | 1 | 7.19 |
| CHEMBL3717944 | — | — | 1 | 7.13 |
| CHEMBL3718425 | — | — | 1 | 7.09 |
| CHEMBL3716057 | GEFAPIXANT | 4.0 | 1 | 7.05 |
| CHEMBL3716384 | — | — | 1 | 7.05 |
| CHEMBL494581 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3715500 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL494161 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL3717153 | — | IC50 | = | 10.23 | nM | 7.99 |
| CHEMBL495204 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL3718862 | — | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL523173 | — | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL3718402 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL492300 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL3716526 | — | Ki | = | 24.55 | nM | 7.61 |
| CHEMBL3715486 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL494159 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL2304566 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL494160 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL494353 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL526307 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL3715231 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL492907 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL3717944 | — | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL3718425 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL3716057 | GEFAPIXANT | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL3716384 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL494581 | — | Ki | = | 851.14 | nM | 6.07 |