Assay Detail
Binding
CHEMBL2428210
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Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay
47
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 47 | 7.16 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426624 | — | — | 2 | 9.52 |
| CHEMBL2426665 | — | — | 1 | 8.85 |
| CHEMBL2426662 | — | — | 1 | 8.62 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.60 |
| CHEMBL2426664 | — | — | 1 | 8.39 |
| CHEMBL2426625 | — | — | 1 | 7.77 |
| CHEMBL2426636 | — | — | 1 | 7.75 |
| CHEMBL2426648 | — | — | 1 | 7.72 |
| CHEMBL2426623 | — | — | 2 | 7.70 |
| CHEMBL2426660 | — | — | 1 | 7.70 |
| CHEMBL1801004 | — | — | 1 | 7.68 |
| CHEMBL2426661 | — | — | 1 | 7.64 |
| CHEMBL2426645 | — | — | 1 | 7.64 |
| CHEMBL2426658 | — | — | 1 | 7.62 |
| CHEMBL2426628 | — | — | 1 | 7.54 |
| CHEMBL2426633 | — | — | 1 | 7.54 |
| CHEMBL2426638 | — | — | 1 | 7.54 |
| CHEMBL2426656 | — | — | 1 | 7.35 |
| CHEMBL2426627 | — | — | 1 | 7.31 |
| CHEMBL2426652 | — | — | 1 | 7.25 |
| CHEMBL2426641 | — | — | 1 | 7.18 |
| CHEMBL2426643 | — | — | 1 | 7.14 |
| CHEMBL2426640 | — | — | 1 | 7.09 |
| CHEMBL2426637 | — | — | 1 | 7.09 |
| CHEMBL2426635 | — | — | 1 | 7.06 |
| CHEMBL2426663 | — | — | 1 | 7.04 |
| CHEMBL2426650 | — | — | 1 | 6.97 |
| CHEMBL2426655 | — | — | 1 | 6.94 |
| CHEMBL2426647 | — | — | 1 | 6.90 |
| CHEMBL2426629 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426624 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2426665 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2426662 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2426664 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2426624 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2426625 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2426636 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2426648 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2426623 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2426660 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1801004 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2426645 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2426661 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2426658 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2426628 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2426633 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2426638 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2426656 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2426627 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2426652 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2426641 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2426643 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2426637 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2426640 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2426635 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2426663 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2426650 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL2426655 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL2426647 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL2426629 | — | EC50 | = | 141.0 | nM | 6.85 |
| CHEMBL2426653 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL2426654 | — | EC50 | = | 301.0 | nM | 6.52 |
| CHEMBL2426649 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL2426642 | — | EC50 | = | 389.0 | nM | 6.41 |
| CHEMBL2426644 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2426623 | — | EC50 | = | 453.0 | nM | 6.34 |
| CHEMBL2426657 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2426659 | — | EC50 | = | 617.0 | nM | 6.21 |
| CHEMBL2426639 | — | EC50 | = | 705.0 | nM | 6.15 |
| CHEMBL2426646 | — | EC50 | = | 956.0 | nM | 6.02 |
| CHEMBL2426630 | — | EC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2426651 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2426631 | — | EC50 | = | 1932.0 | nM | 5.71 |
| CHEMBL2426634 | — | EC50 | = | 4322.0 | nM | 5.36 |
| CHEMBL2426626 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426632 | — | EC50 | > | 10000.0 | nM | - |