Assay Detail
Functional
CHEMBL4011248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Potent and Selective Antagonists for the UTP-Activated P2Y4 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 65 | 5.50 | 6.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4087247 | — | — | 1 | 6.63 |
| CHEMBL4094930 | — | — | 1 | 6.43 |
| CHEMBL4081274 | — | — | 1 | 6.40 |
| CHEMBL4090874 | — | — | 1 | 6.39 |
| CHEMBL4099292 | — | — | 1 | 6.32 |
| CHEMBL1365553 | — | — | 1 | 6.20 |
| CHEMBL4069492 | — | — | 1 | 6.13 |
| CHEMBL223344 | RB 2 | — | 1 | 5.94 |
| CHEMBL496620 | — | — | 1 | 5.93 |
| CHEMBL1671997 | — | — | 1 | 5.86 |
| CHEMBL1671993 | — | — | 1 | 5.82 |
| CHEMBL4090513 | — | — | 1 | 5.81 |
| CHEMBL4082692 | — | — | 1 | 5.78 |
| CHEMBL4074456 | — | — | 1 | 5.77 |
| CHEMBL1671995 | — | — | 1 | 5.77 |
| CHEMBL4065831 | — | — | 1 | 5.75 |
| CHEMBL401859 | — | — | 1 | 5.72 |
| CHEMBL597203 | — | — | 1 | 5.71 |
| CHEMBL256057 | ACID BLUE 25 | — | 1 | 5.71 |
| CHEMBL4060811 | — | — | 1 | 5.66 |
| CHEMBL445413 | — | — | 1 | 5.65 |
| CHEMBL271672 | — | — | 1 | 5.63 |
| CHEMBL401735 | — | — | 1 | 5.59 |
| CHEMBL402239 | — | — | 1 | 5.58 |
| CHEMBL522053 | — | — | 1 | 5.56 |
| CHEMBL404450 | — | — | 1 | 5.55 |
| CHEMBL4063945 | — | — | 1 | 5.52 |
| CHEMBL271673 | — | — | 1 | 5.52 |
| CHEMBL496030 | — | — | 1 | 5.50 |
| CHEMBL4078095 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4087247 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL4094930 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL4081274 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4090874 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL4099292 | — | IC50 | = | 482.0 | nM | 6.32 |
| CHEMBL1365553 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL4069492 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL223344 | RB 2 | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL496620 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL1671997 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL1671993 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL4090513 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL4082692 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL1671995 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4074456 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL4065831 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL401859 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL597203 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL256057 | ACID BLUE 25 | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4060811 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL445413 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL271672 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL401735 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL402239 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL522053 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL404450 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL271673 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL4063945 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL496030 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL4078095 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL599050 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4081964 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL495605 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL256864 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL256688 | — | IC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL402238 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL257495 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL604158 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL4072198 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL4063599 | — | IC50 | = | 4980.0 | nM | 5.30 |
| CHEMBL524064 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL1671994 | — | IC50 | = | 6450.0 | nM | 5.19 |
| CHEMBL1672098 | — | IC50 | = | 6960.0 | nM | 5.16 |
| CHEMBL498224 | — | IC50 | = | 7180.0 | nM | 5.14 |
| CHEMBL498423 | — | IC50 | = | 7420.0 | nM | 5.13 |
| CHEMBL1671996 | — | IC50 | = | 9250.0 | nM | 5.03 |
| CHEMBL4084432 | — | IC50 | = | 9340.0 | nM | 5.03 |
| CHEMBL256689 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL1672099 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL498223 | — | IC50 | = | 14400.0 | nM | 4.84 |