Assay Detail
Binding
CHEMBL872288
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Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.02 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.10 |
| CHEMBL197268 | — | — | 1 | 6.29 |
| CHEMBL198170 | — | — | 1 | 6.24 |
| CHEMBL198166 | — | — | 1 | 6.16 |
| CHEMBL198708 | — | — | 1 | 6.14 |
| CHEMBL383607 | — | — | 1 | 6.02 |
| CHEMBL199121 | — | — | 1 | 6.01 |
| CHEMBL2113107 | — | — | 1 | 5.99 |
| CHEMBL194698 | — | — | 1 | 5.98 |
| CHEMBL2113106 | — | — | 1 | 5.88 |
| CHEMBL2113109 | — | — | 1 | 5.54 |
| CHEMBL2113104 | — | — | 1 | 5.42 |
| CHEMBL198163 | — | — | 1 | 5.36 |
| CHEMBL196261 | — | — | 1 | 5.17 |
| CHEMBL2113108 | — | — | 1 | - |
| CHEMBL373318 | — | — | 1 | - |
| CHEMBL370374 | — | — | 1 | - |
| CHEMBL199125 | — | — | 1 | - |
| CHEMBL197684 | — | — | 1 | - |
| CHEMBL198034 | — | — | 1 | - |
| CHEMBL196260 | — | — | 1 | - |
| CHEMBL2113105 | — | — | 1 | - |
| CHEMBL196227 | — | — | 1 | - |
| CHEMBL196139 | — | — | 1 | - |
| CHEMBL199172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL197268 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL198170 | — | Ki | = | 579.0 | nM | 6.24 |
| CHEMBL198166 | — | Ki | = | 695.0 | nM | 6.16 |
| CHEMBL198708 | — | Ki | = | 718.0 | nM | 6.14 |
| CHEMBL383607 | — | Ki | = | 947.0 | nM | 6.02 |
| CHEMBL199121 | — | Ki | = | 969.0 | nM | 6.01 |
| CHEMBL2113107 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL194698 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL2113106 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL2113109 | — | Ki | = | 2860.0 | nM | 5.54 |
| CHEMBL2113104 | — | Ki | = | 3760.0 | nM | 5.42 |
| CHEMBL198163 | — | Ki | = | 4390.0 | nM | 5.36 |
| CHEMBL196261 | — | Ki | = | 6690.0 | nM | 5.17 |
| CHEMBL2113108 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL373318 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL370374 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL199125 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL197684 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL198034 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL196260 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2113105 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL196227 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL196139 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL199172 | — | Ki | > | 10000.0 | nM | - |