Assay Detail
Binding
CHEMBL1114665
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Binding affinity to human glucocorticoid receptor by fluorescence polarization competitive binding assay
22
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-Functionalized indazoles as glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.91 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.15 |
| CHEMBL1094209 | — | — | 1 | 7.85 |
| CHEMBL1094536 | — | — | 1 | 7.52 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 2 | 7.47 |
| CHEMBL1094207 | — | — | 1 | 7.46 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 2 | 7.31 |
| CHEMBL1095228 | — | — | 1 | 7.28 |
| CHEMBL1094206 | — | — | 1 | 7.27 |
| CHEMBL1096467 | — | — | 1 | 7.27 |
| CHEMBL1094514 | — | — | 1 | 7.23 |
| CHEMBL1094526 | — | — | 1 | 7.14 |
| CHEMBL1095541 | 2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) | — | 3 | 7.07 |
| CHEMBL1094527 | — | — | 1 | 7.00 |
| CHEMBL1095227 | — | — | 1 | 6.75 |
| CHEMBL1096126 | — | — | 1 | 6.55 |
| CHEMBL1098849 | — | — | 1 | 5.68 |
| CHEMBL1097475 | — | — | 1 | 5.67 |
| CHEMBL1095542 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1094209 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1094536 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1094207 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1095228 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1096467 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1094206 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1094514 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1094526 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1095541 | 2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1094527 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1095541 | 2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL1095227 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL1096126 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL1098849 | — | IC50 | = | 2089.0 | nM | 5.68 |
| CHEMBL1097475 | — | IC50 | = | 2113.0 | nM | 5.67 |
| CHEMBL1095541 | 2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1095542 | — | IC50 | = | 10000.0 | nM | 5.00 |