Assay Detail
Binding
CHEMBL3706350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Lanthascreen Competitive Binding Assay: The assay was performed according to manufacturer protocol. A mixture of 5 nM GST-PPARG-LBD, 5 nM Tb-GST-antibody, 5 nM Fluormone Pan- PPAR Green, and serial dilutions of the experimental compound, beginning at 10 μΜ downwards, was added to wells of black 384-well low- volume plates (Greiner) to a total volume of 18 xL. All dilutions were made in TR-FRET assay buffer C. DMSO at 2% final concentration was used as a no-ligand control. Experiment was performed in triplicate, and incubated for 2 hours in the dark prior to assay read in Perkin Elmer ViewLux ultra HTS microplate reader. FRET signal was measured by excitation at 340 nm and emission at 520 nm for fluorescein and 490 nm for terbium.
89
Total Activities
85
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 |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-benzylindole modulators of PPARG
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 89 | 7.41 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3678131 | — | — | 1 | 10.22 |
| CHEMBL3678128 | — | — | 2 | 9.70 |
| CHEMBL3678134 | — | — | 2 | 9.70 |
| CHEMBL3678133 | — | — | 1 | 9.52 |
| CHEMBL3678126 | — | — | 1 | 9.22 |
| CHEMBL3678125 | — | — | 1 | 9.22 |
| CHEMBL3678132 | — | — | 1 | 9.22 |
| CHEMBL3678127 | — | — | 1 | 9.15 |
| CHEMBL3678086 | — | — | 1 | 9.00 |
| CHEMBL3678129 | — | — | 1 | 8.80 |
| CHEMBL3678135 | — | — | 1 | 8.80 |
| CHEMBL3678106 | — | — | 1 | 8.52 |
| CHEMBL3678089 | — | — | 1 | 8.40 |
| CHEMBL3678087 | — | — | 1 | 8.30 |
| CHEMBL3678130 | — | — | 1 | 8.30 |
| CHEMBL3678136 | — | — | 1 | 8.30 |
| CHEMBL3678090 | — | — | 1 | 8.15 |
| CHEMBL3678105 | — | — | 1 | 8.15 |
| CHEMBL3678085 | — | — | 1 | 8.05 |
| CHEMBL3678158 | — | — | 1 | 8.00 |
| CHEMBL3678161 | — | — | 1 | 7.89 |
| CHEMBL3678093 | — | — | 1 | 7.85 |
| CHEMBL3678159 | — | — | 1 | 7.80 |
| CHEMBL3678160 | — | — | 1 | 7.70 |
| CHEMBL3678146 | — | — | 2 | 7.62 |
| CHEMBL3678140 | — | — | 1 | 7.60 |
| CHEMBL3678099 | — | — | 1 | 7.54 |
| CHEMBL3678137 | — | — | 1 | 7.51 |
| CHEMBL3678088 | — | — | 1 | 7.51 |
| CHEMBL3678162 | — | — | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3678131 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3678128 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678134 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678133 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3678126 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3678125 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3678132 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3678127 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3678086 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3678129 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3678135 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3678106 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3678089 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3678130 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678087 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678136 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678090 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3678105 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3678085 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3678158 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3678161 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3678093 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3678159 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3678160 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3678146 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3678140 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3678099 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3678137 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3678088 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3678162 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3678155 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3678107 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3678092 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3678111 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3678118 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3678149 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3678117 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3678156 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3678153 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3678141 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3678112 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3678157 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3678121 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3678116 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3678139 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3678163 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3678150 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3678154 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3678147 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3678104 | — | IC50 | = | 98.0 | nM | 7.01 |