Assay Detail
Functional
CHEMBL1037628
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Antagonist activity at human T1R2/T1R3 receptor expressed in HEK293E cells assessed as inhibition of sucralose-induced intracellular calcium mobilization
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293E |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Phenoxy herbicides and fibrates potently inhibit the human chemosensory receptor subunit T1R3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.58 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573221 | RAC-DICHLORPROP | — | 1 | 5.28 |
| CHEMBL460296 | FENOPROP | — | 1 | 5.24 |
| CHEMBL272942 | MECOPROP | — | 1 | 4.92 |
| CHEMBL683 | CLOFIBRIC ACID | 2.0 | 1 | 4.55 |
| CHEMBL367623 | 2,4-DICHLOROPHENOXYACETIC ACID | — | 1 | 4.30 |
| CHEMBL573448 | LACTISOLE | 1.0 | 1 | 4.16 |
| CHEMBL457 | GEMFIBROZIL | 4.0 | 1 | 4.16 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.00 |
| CHEMBL207225 | INDOLYLPROPIONIC ACID | — | 1 | - |
| CHEMBL82411 | INDOLE-3-ACETIC ACID | — | 1 | - |
| CHEMBL582878 | — | — | 1 | - |
| CHEMBL1044 | PHENYLACETIC ACID | -1.0 | 1 | - |
| CHEMBL428495 | — | — | 1 | - |
| CHEMBL178018 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573221 | RAC-DICHLORPROP | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL460296 | FENOPROP | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL272942 | MECOPROP | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL683 | CLOFIBRIC ACID | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL367623 | 2,4-DICHLOROPHENOXYACETIC ACID | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL573448 | LACTISOLE | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL457 | GEMFIBROZIL | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL264374 | BEZAFIBRATE | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL207225 | INDOLYLPROPIONIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL82411 | INDOLE-3-ACETIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL582878 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1044 | PHENYLACETIC ACID | IC50 | > | 500000.0 | nM | - |
| CHEMBL428495 | — | IC50 | = | 233000.0 | nM | - |
| CHEMBL178018 | — | IC50 | = | 142000.0 | nM | - |