Assay Detail
Functional
CHEMBL960837
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant P2X2/3 receptor expressed in human 1321N1 cells by FLIPR assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
P2X2/P2X3 heterotrimeric receptor (CHEMBL3831281) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.22 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495204 | — | — | 1 | 7.90 |
| CHEMBL526307 | — | — | 1 | 7.10 |
| CHEMBL495203 | — | — | 1 | 7.10 |
| CHEMBL448525 | — | — | 1 | 7.00 |
| CHEMBL502618 | — | — | 1 | 6.80 |
| CHEMBL444469 | — | — | 1 | 6.80 |
| CHEMBL521983 | — | — | 1 | 6.50 |
| CHEMBL500550 | — | — | 1 | 6.50 |
| CHEMBL523043 | — | — | 1 | 6.50 |
| CHEMBL504607 | — | — | 1 | 6.40 |
| CHEMBL446310 | — | — | 1 | 6.40 |
| CHEMBL494176 | — | — | 1 | 6.40 |
| CHEMBL494833 | — | — | 1 | 6.30 |
| CHEMBL492968 | — | — | 1 | 6.20 |
| CHEMBL492967 | — | — | 1 | 6.00 |
| CHEMBL521820 | — | — | 1 | 5.80 |
| CHEMBL494940 | — | — | 1 | 5.80 |
| CHEMBL494834 | — | — | 1 | 5.70 |
| CHEMBL494181 | — | — | 1 | 5.70 |
| CHEMBL494832 | — | — | 1 | 5.70 |
| CHEMBL494772 | — | — | 1 | 5.70 |
| CHEMBL492562 | — | — | 1 | 5.60 |
| CHEMBL495195 | — | — | 1 | 5.60 |
| CHEMBL522184 | — | — | 1 | 5.10 |
| CHEMBL494240 | — | — | 1 | 5.00 |
| CHEMBL494239 | — | — | 1 | - |
| CHEMBL495370 | — | — | 1 | - |
| CHEMBL494760 | ORMETOPRIM | 2.0 | 1 | - |
| CHEMBL494849 | — | — | 1 | - |
| CHEMBL494761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495204 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL526307 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL495203 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL448525 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL502618 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL444469 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL521983 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL500550 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL523043 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL446310 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL494176 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL504607 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL494833 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL492968 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL492967 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL521820 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL494940 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL494772 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL494181 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL494834 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL494832 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL492562 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL495195 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL522184 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL494240 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL524043 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL510124 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492788 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492787 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492786 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494761 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494849 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494760 | ORMETOPRIM | IC50 | > | 10000.0 | nM | - |
| CHEMBL495370 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494239 | — | IC50 | > | 10000.0 | nM | - |