Assay Detail
Functional
CHEMBL4722342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Uracil nucleotide/cysteinyl leukotriene receptor (CHEMBL1075162) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of suramin-derived dual antagonists of the proinflammatory G protein-coupled receptors P2Y and GPR17.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.47 | 5.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748101 | — | — | 1 | 5.88 |
| CHEMBL4752357 | — | — | 1 | 5.80 |
| CHEMBL4748522 | — | — | 1 | 5.78 |
| CHEMBL4743510 | — | — | 1 | 5.78 |
| CHEMBL4780920 | — | — | 1 | 5.72 |
| CHEMBL4777444 | — | — | 1 | 5.63 |
| CHEMBL4743246 | — | — | 1 | 5.52 |
| CHEMBL4750852 | — | — | 1 | 5.51 |
| CHEMBL4796857 | — | — | 1 | 5.50 |
| CHEMBL4783980 | — | — | 1 | 5.48 |
| CHEMBL4753843 | — | — | 1 | 5.47 |
| CHEMBL4797060 | — | — | 1 | 5.44 |
| CHEMBL4764999 | — | — | 1 | 5.41 |
| CHEMBL4799394 | — | — | 1 | 5.39 |
| CHEMBL4741242 | — | — | 1 | 5.38 |
| CHEMBL4741688 | — | — | 1 | 5.33 |
| CHEMBL4758186 | — | — | 1 | 5.24 |
| CHEMBL4756398 | — | — | 1 | 5.21 |
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | 4.54 |
| CHEMBL4751881 | — | — | 1 | - |
| CHEMBL413376 | SURAMIN HEXASODIUM | 3.0 | 1 | - |
| CHEMBL4082045 | — | — | 1 | - |
| CHEMBL4796940 | — | — | 1 | - |
| CHEMBL4748357 | — | — | 1 | - |
| CHEMBL4755321 | — | — | 1 | - |
| CHEMBL4786643 | — | — | 1 | - |
| CHEMBL4782488 | — | — | 1 | - |
| CHEMBL4784624 | — | — | 1 | - |
| CHEMBL4796055 | — | — | 1 | - |
| CHEMBL4786491 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748101 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4752357 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4748522 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL4743510 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL4780920 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL4777444 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4743246 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4750852 | — | IC50 | = | 3060.0 | nM | 5.51 |
| CHEMBL4796857 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4783980 | — | IC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL4753843 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL4797060 | — | IC50 | = | 3610.0 | nM | 5.44 |
| CHEMBL4764999 | — | IC50 | = | 3880.0 | nM | 5.41 |
| CHEMBL4799394 | — | IC50 | = | 4070.0 | nM | 5.39 |
| CHEMBL4741242 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL4741688 | — | IC50 | = | 4620.0 | nM | 5.33 |
| CHEMBL4758186 | — | IC50 | = | 5750.0 | nM | 5.24 |
| CHEMBL4756398 | — | IC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL6 | INDOMETHACIN | IC50 | = | 28800.0 | nM | 4.54 |
| CHEMBL4751650 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4763168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4742739 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4763683 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4762760 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4795664 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4753686 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4750327 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4758622 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4786491 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4796055 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4784624 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4782488 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4786643 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4755321 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4748357 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL4796940 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4082045 | — | IC50 | - | — | - | |
| CHEMBL413376 | SURAMIN HEXASODIUM | IC50 | > | 100000.0 | nM | - |
| CHEMBL4751881 | — | IC50 | > | 10000.0 | nM | - |