Assay Detail
Binding
CHEMBL3868161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduction in PMA-stimulated TRE-LacZ activity after 24 hrs in presence of MUG by fluorometric assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | ChaGo-K-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.90 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3911831 | — | — | 1 | 10.52 |
| CHEMBL3973775 | — | — | 1 | 10.40 |
| CHEMBL3902818 | — | — | 1 | 10.40 |
| CHEMBL3920760 | — | — | 1 | 10.30 |
| CHEMBL3901719 | — | — | 1 | 10.10 |
| CHEMBL3960682 | — | — | 1 | 10.05 |
| CHEMBL3940724 | — | — | 1 | 10.05 |
| CHEMBL3915997 | — | — | 1 | 9.89 |
| CHEMBL3892759 | — | — | 1 | 9.68 |
| CHEMBL3935790 | — | — | 1 | 9.60 |
| CHEMBL3937635 | — | — | 1 | 9.40 |
| CHEMBL3893393 | — | — | 1 | 9.33 |
| CHEMBL3897280 | — | — | 1 | 9.21 |
| CHEMBL3901337 | — | — | 1 | 9.21 |
| CHEMBL3970276 | — | — | 1 | 9.18 |
| CHEMBL3976935 | — | — | 1 | 9.12 |
| CHEMBL3964502 | — | — | 1 | 9.08 |
| CHEMBL3914142 | — | — | 1 | 9.04 |
| CHEMBL3962413 | — | — | 1 | 8.94 |
| CHEMBL3977631 | — | — | 1 | 8.85 |
| CHEMBL3899942 | — | — | 1 | 8.85 |
| CHEMBL3261407 | — | — | 1 | 8.83 |
| CHEMBL3932081 | — | — | 1 | 8.55 |
| CHEMBL3934504 | — | — | 1 | 8.51 |
| CHEMBL3907432 | — | — | 1 | 8.29 |
| CHEMBL3970640 | — | — | 1 | 8.18 |
| CHEMBL3923131 | — | — | 1 | 8.13 |
| CHEMBL3967290 | — | — | 1 | 8.05 |
| CHEMBL3945990 | — | — | 1 | 7.96 |
| CHEMBL3933196 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3911831 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3973775 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3902818 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3920760 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3901719 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3960682 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3940724 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3915997 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3892759 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL3935790 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3937635 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3893393 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL3897280 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL3901337 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL3970276 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL3976935 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3964502 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL3914142 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL3962413 | — | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL3977631 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3899942 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL3261407 | — | IC50 | = | 1.47 | nM | 8.83 |
| CHEMBL3932081 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3934504 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3907432 | — | IC50 | = | 5.09 | nM | 8.29 |
| CHEMBL3970640 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3923131 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL3967290 | — | IC50 | = | 8.83 | nM | 8.05 |
| CHEMBL3945990 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3933196 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3959591 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3963259 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3261406 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3963321 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3906238 | — | IC50 | = | 100.0 | nM | 7.00 |