Assay Detail
Binding
CHEMBL4324752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X4 receptor tranfected in HEK293 cells assessed as inhibition of Bz-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor <i>N</i>-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.06 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452312 | — | — | 1 | 8.70 |
| CHEMBL4471140 | — | — | 1 | 8.70 |
| CHEMBL4589444 | — | — | 1 | 8.30 |
| CHEMBL4579583 | — | — | 1 | 8.10 |
| CHEMBL4447043 | — | — | 1 | 8.05 |
| CHEMBL4522504 | — | — | 1 | 8.00 |
| CHEMBL4556573 | — | — | 1 | 8.00 |
| CHEMBL4555657 | — | — | 1 | 7.89 |
| CHEMBL4516176 | — | — | 1 | 7.89 |
| CHEMBL4521017 | — | — | 1 | 7.82 |
| CHEMBL4563994 | — | — | 1 | 7.72 |
| CHEMBL4438327 | — | — | 1 | 7.62 |
| CHEMBL4439570 | — | — | 1 | 7.58 |
| CHEMBL4535761 | — | — | 1 | 7.57 |
| CHEMBL4463320 | — | — | 1 | 7.52 |
| CHEMBL4517831 | — | — | 1 | 7.43 |
| CHEMBL4539658 | — | — | 1 | 7.41 |
| CHEMBL4474747 | — | — | 1 | 7.35 |
| CHEMBL4443234 | — | — | 1 | 7.28 |
| CHEMBL4438981 | — | — | 1 | 7.17 |
| CHEMBL4516450 | — | — | 1 | 7.12 |
| CHEMBL4561582 | — | — | 1 | 7.12 |
| CHEMBL4452251 | — | — | 1 | 7.08 |
| CHEMBL4519162 | — | — | 1 | 7.06 |
| CHEMBL4449416 | — | — | 1 | 7.04 |
| CHEMBL4579675 | — | — | 1 | 7.03 |
| CHEMBL4469574 | — | — | 1 | 6.96 |
| CHEMBL4593104 | — | — | 1 | 6.87 |
| CHEMBL4442297 | — | — | 1 | 6.86 |
| CHEMBL4451946 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452312 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4471140 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4589444 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4579583 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4447043 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4522504 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4556573 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4555657 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4516176 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4521017 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4563994 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4438327 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4439570 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4535761 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4463320 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4517831 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4539658 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4474747 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4443234 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4438981 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4516450 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4561582 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4452251 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4519162 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4449416 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4579675 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4469574 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL4593104 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4442297 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4451946 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4443857 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL4462109 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4541425 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4521594 | BAY-1797 | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4577125 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4450002 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL4450779 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4451276 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL4444721 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL4539332 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL4533763 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL4455317 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL4458990 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL4456686 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL4470995 | — | IC50 | = | 1242.0 | nM | 5.91 |
| CHEMBL4470126 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4569107 | — | IC50 | = | 1681.0 | nM | 5.77 |
| CHEMBL4570116 | — | IC50 | = | 1718.0 | nM | 5.76 |
| CHEMBL4455389 | — | IC50 | = | 2528.0 | nM | 5.60 |
| CHEMBL4516843 | BAY-207 | IC50 | > | 25000.0 | nM | - |