Assay Detail
Binding
CHEMBL760250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)
36
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.29 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 8.94 |
| CHEMBL434063 | — | — | 2 | 8.85 |
| CHEMBL423026 | — | — | 1 | 8.83 |
| CHEMBL146822 | — | — | 1 | 8.48 |
| CHEMBL147826 | — | — | 1 | 8.43 |
| CHEMBL59132 | — | — | 1 | 8.37 |
| CHEMBL358137 | — | — | 1 | 8.29 |
| CHEMBL148301 | — | — | 1 | 8.28 |
| CHEMBL346219 | — | — | 1 | 8.19 |
| CHEMBL356350 | — | — | 2 | 7.93 |
| CHEMBL17805 | BRL-48482 | — | 1 | 7.57 |
| CHEMBL146614 | — | — | 1 | 7.55 |
| CHEMBL147694 | — | — | 1 | 7.49 |
| CHEMBL146322 | — | — | 1 | 7.48 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.33 |
| CHEMBL357479 | — | — | 1 | 7.29 |
| CHEMBL148060 | — | — | 1 | 7.07 |
| CHEMBL146123 | — | — | 1 | 6.91 |
| CHEMBL359377 | — | — | 1 | 6.79 |
| CHEMBL145829 | — | — | 1 | 6.79 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 6.52 |
| CHEMBL144877 | — | — | 1 | 6.12 |
| CHEMBL346415 | — | — | 1 | 6.10 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 5.91 |
| CHEMBL147042 | — | — | 1 | 5.90 |
| CHEMBL146201 | — | — | 1 | 5.88 |
| CHEMBL145929 | — | — | 1 | 5.71 |
| CHEMBL7002 | CIGLITAZONE | 2.0 | 1 | 5.51 |
| CHEMBL147608 | — | — | 1 | - |
| CHEMBL146243 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107367 | FARGLITAZAR | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL434063 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL423026 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL146822 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL147826 | — | Ki | = | 3.715 | nM | 8.43 |
| CHEMBL59132 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL358137 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL148301 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL346219 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL356350 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL17805 | BRL-48482 | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL146614 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL147694 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL146322 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL121 | ROSIGLITAZONE | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL357479 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL148060 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL434063 | — | Ki | = | 104.71 | nM | 6.98 |
| CHEMBL146123 | — | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL359377 | — | Ki | = | 162.18 | nM | 6.79 |
| CHEMBL145829 | — | Ki | = | 162.18 | nM | 6.79 |
| CHEMBL408 | TROGLITAZONE | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL144877 | — | Ki | = | 758.58 | nM | 6.12 |
| CHEMBL346415 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL595 | PIOGLITAZONE | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL147042 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL146201 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL145929 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL7002 | CIGLITAZONE | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL147608 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL146243 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL146027 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL342512 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL358298 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL149609 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL356350 | — | Ki | < | 3162.28 | nM | - |