Assay Detail
Functional
CHEMBL1073135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 receptor expressed in human U2-OS cells assessed as changes in response to cAMP level by MRE/CRE-driven luciferase reporter gene assay
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 66 | 6.65 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL612138 | — | — | 1 | 9.00 |
| CHEMBL601638 | — | — | 1 | 8.40 |
| CHEMBL603112 | — | — | 1 | 8.40 |
| CHEMBL601440 | — | — | 1 | 8.10 |
| CHEMBL605367 | — | — | 1 | 8.00 |
| CHEMBL601637 | — | — | 1 | 8.00 |
| CHEMBL590495 | — | — | 1 | 7.90 |
| CHEMBL604131 | — | — | 1 | 7.90 |
| CHEMBL601441 | — | — | 1 | 7.90 |
| CHEMBL600821 | — | — | 1 | 7.90 |
| CHEMBL604537 | — | — | 1 | 7.90 |
| CHEMBL600827 | — | — | 1 | 7.80 |
| CHEMBL598743 | — | — | 1 | 7.70 |
| CHEMBL601882 | — | — | 1 | 7.70 |
| CHEMBL599328 | — | — | 1 | 7.70 |
| CHEMBL603921 | — | — | 1 | 7.70 |
| CHEMBL604543 | — | — | 1 | 7.50 |
| CHEMBL600833 | — | — | 1 | 7.50 |
| CHEMBL575966 | — | — | 1 | 7.50 |
| CHEMBL600834 | — | — | 1 | 7.40 |
| CHEMBL601428 | — | — | 1 | 7.20 |
| CHEMBL600020 | — | — | 1 | 7.20 |
| CHEMBL603500 | — | — | 1 | 7.20 |
| CHEMBL576138 | — | — | 1 | 7.10 |
| CHEMBL602892 | — | — | 1 | 7.10 |
| CHEMBL590982 | — | — | 1 | 7.00 |
| CHEMBL600421 | — | — | 1 | 6.90 |
| CHEMBL600629 | — | — | 1 | 6.90 |
| CHEMBL601233 | — | — | 1 | 6.80 |
| CHEMBL600021 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL612138 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL601638 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL603112 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL601440 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL605367 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL601637 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL590495 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL604131 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL601441 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL600821 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL604537 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL600827 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL601882 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL598743 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL599328 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL603921 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL604543 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL600833 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL575966 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL600834 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL601428 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL600020 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL603500 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL576138 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL602892 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL590982 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL600629 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL600421 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL601233 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL600021 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL599347 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL602691 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL608867 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL605356 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL605986 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL604751 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL591455 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL601449 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL590739 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL601670 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL591927 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL604752 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL592645 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL603096 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL599126 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL600410 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL600422 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL599127 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL592158 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL603706 | — | EC50 | = | 1258.93 | nM | 5.90 |