Assay Detail
Binding
CHEMBL5129286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as inhibition of EA-evoked Calcium influx by measuring reduction in intracellular Ca2+ level and measured upto 360 sec by Fluo-4/AM dye based FLIPR assay
36
Total Activities
36
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 |
Target
Short transient receptor potential channel 5 (CHEMBL1250411) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.71 | 6.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5207902 | — | — | 1 | 6.27 |
| CHEMBL5201191 | — | — | 1 | 6.24 |
| CHEMBL5190035 | — | — | 1 | 6.17 |
| CHEMBL5169865 | — | — | 1 | 6.09 |
| CHEMBL5203265 | — | — | 1 | 6.04 |
| CHEMBL5209321 | — | — | 1 | 6.02 |
| CHEMBL5186222 | — | — | 1 | 5.99 |
| CHEMBL5201859 | — | — | 1 | 5.87 |
| CHEMBL5173485 | — | — | 1 | 5.87 |
| CHEMBL5183590 | — | — | 1 | 5.74 |
| CHEMBL5187515 | — | — | 1 | 5.66 |
| CHEMBL5192702 | — | — | 1 | 5.66 |
| CHEMBL5171565 | — | — | 1 | 5.65 |
| CHEMBL5194092 | — | — | 1 | 5.64 |
| CHEMBL5206434 | — | — | 1 | 5.64 |
| CHEMBL5202944 | — | — | 1 | 5.62 |
| CHEMBL5182312 | — | — | 1 | 5.58 |
| CHEMBL5202586 | — | — | 1 | 5.53 |
| CHEMBL5194160 | — | — | 1 | 5.53 |
| CHEMBL5176140 | — | — | 1 | 5.50 |
| CHEMBL5185813 | — | — | 1 | 5.47 |
| CHEMBL5191462 | — | — | 1 | 5.33 |
| CHEMBL1345058 | — | — | 1 | 4.19 |
| CHEMBL5191534 | — | — | 1 | - |
| CHEMBL5186146 | — | — | 1 | - |
| CHEMBL5185490 | — | — | 1 | - |
| CHEMBL5173272 | — | — | 1 | - |
| CHEMBL5172936 | — | — | 1 | - |
| CHEMBL5170000 | — | — | 1 | - |
| CHEMBL5195015 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5207902 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5201191 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5190035 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5169865 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5203265 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5209321 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL5186222 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5201859 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL5173485 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL5183590 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL5187515 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL5192702 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL5171565 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL5194092 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL5206434 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5202944 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL5182312 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL5194160 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL5202586 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL5176140 | — | IC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL5185813 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL5191462 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL1345058 | — | IC50 | = | 64970.0 | nM | 4.19 |
| CHEMBL5206422 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5169949 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5200061 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5208734 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5200070 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5182054 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5195015 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5170000 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5172936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5173272 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5185490 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5186146 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5191534 | — | IC50 | > | 10000.0 | nM | - |