Assay Detail
Binding
CHEMBL3887982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Use of fenoterol and fenoterol analogues in the treatment of glioblastomas and astrocytomas
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.32 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1160723 | LEVISOPRENALINE | 2.0 | 1 | 10.30 |
| CHEMBL388570 | — | — | 1 | 9.85 |
| CHEMBL228992 | — | — | 1 | 9.77 |
| CHEMBL229614 | — | — | 1 | 8.92 |
| CHEMBL1800936 | — | — | 1 | 8.84 |
| CHEMBL229401 | — | — | 2 | 8.80 |
| CHEMBL1800961 | — | — | 1 | 8.72 |
| CHEMBL228996 | — | — | 1 | 8.70 |
| CHEMBL228998 | — | — | 1 | 8.50 |
| CHEMBL1800963 | — | — | 1 | 8.40 |
| CHEMBL1800934 | — | — | 1 | 8.36 |
| CHEMBL229476 | — | — | 1 | 8.21 |
| CHEMBL229477 | — | — | 1 | 8.17 |
| CHEMBL388177 | — | — | 1 | 7.83 |
| CHEMBL1800960 | — | — | 1 | 7.75 |
| CHEMBL1800962 | — | — | 1 | 7.14 |
| CHEMBL389390 | — | — | 1 | 6.74 |
| CHEMBL228417 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1160723 | LEVISOPRENALINE | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL388570 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL228992 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL229614 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL1800936 | — | IC50 | = | 1.44 | nM | 8.84 |
| CHEMBL229401 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL1800961 | — | IC50 | = | 1.91 | nM | 8.72 |
| CHEMBL228996 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL228998 | — | IC50 | = | 3.16 | nM | 8.50 |
| CHEMBL1800963 | — | IC50 | = | 3.98 | nM | 8.40 |
| CHEMBL1800934 | — | IC50 | = | 4.37 | nM | 8.36 |
| CHEMBL229476 | — | IC50 | = | 6.09 | nM | 8.21 |
| CHEMBL229477 | — | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL388177 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL1800960 | — | IC50 | = | 17.88 | nM | 7.75 |
| CHEMBL1800962 | — | IC50 | = | 72.6 | nM | 7.14 |
| CHEMBL389390 | — | IC50 | = | 184.2 | nM | 6.74 |
| CHEMBL229401 | — | IC50 | = | 229.1 | nM | 6.64 |
| CHEMBL228417 | — | IC50 | = | 337.2 | nM | 6.47 |