Assay Detail
Functional
CHEMBL899636
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
29
Total Activities
27
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 16 | - | - |
| EC50 | 10 | 5.03 | 6.14 |
| Log EC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL393064 | — | — | 2 | 6.14 |
| CHEMBL235230 | — | — | 2 | 5.49 |
| CHEMBL393065 | — | — | 1 | 5.12 |
| CHEMBL428730 | — | — | 1 | 4.93 |
| CHEMBL397055 | — | — | 1 | 4.91 |
| CHEMBL247921 | — | — | 1 | 4.73 |
| CHEMBL238002 | — | — | 1 | 4.38 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 4.12 |
| CHEMBL128679 | — | — | 1 | - |
| CHEMBL397056 | — | — | 1 | - |
| CHEMBL236728 | — | — | 1 | - |
| CHEMBL235231 | — | — | 1 | - |
| CHEMBL235010 | — | — | 1 | - |
| CHEMBL393062 | — | — | 1 | - |
| CHEMBL235009 | — | — | 1 | - |
| CHEMBL392859 | — | — | 1 | - |
| CHEMBL396864 | — | — | 1 | - |
| CHEMBL238004 | — | — | 1 | - |
| CHEMBL415261 | — | — | 1 | - |
| CHEMBL245491 | — | — | 1 | - |
| CHEMBL237788 | — | — | 1 | - |
| CHEMBL394498 | — | — | 1 | - |
| CHEMBL391574 | — | — | 1 | - |
| CHEMBL393063 | — | — | 1 | - |
| CHEMBL235229 | — | — | 1 | - |
| CHEMBL235228 | — | — | 1 | - |
| CHEMBL247098 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL393064 | — | EC50 | = | 724.44 | nM | 6.14 |
| CHEMBL235230 | — | EC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL235230 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL393065 | — | EC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL428730 | — | EC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL397055 | — | EC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL247921 | — | EC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL238002 | — | EC50 | = | 41686.94 | nM | 4.38 |
| CHEMBL573 | NIACIN | EC50 | = | 75857.76 | nM | 4.12 |
| CHEMBL238004 | — | Activity | - | — | - | |
| CHEMBL396864 | — | Activity | - | — | - | |
| CHEMBL392859 | — | Activity | - | — | - | |
| CHEMBL235009 | — | Activity | - | — | - | |
| CHEMBL393062 | — | Activity | - | — | - | |
| CHEMBL235010 | — | Activity | - | — | - | |
| CHEMBL235231 | — | Activity | - | — | - | |
| CHEMBL236728 | — | Activity | - | — | - | |
| CHEMBL397056 | — | Activity | - | — | - | |
| CHEMBL128679 | — | Activity | - | — | - | |
| CHEMBL415261 | — | Activity | - | — | - | |
| CHEMBL245491 | — | Activity | - | — | - | |
| CHEMBL247098 | — | Activity | - | — | - | |
| CHEMBL394498 | — | Activity | - | — | - | |
| CHEMBL391574 | — | Activity | - | — | - | |
| CHEMBL393063 | — | Log EC50 | - | — | - | |
| CHEMBL235229 | — | Log EC50 | - | — | - | |
| CHEMBL235228 | — | Log EC50 | - | — | - | |
| CHEMBL393064 | — | EC50 | = | 860000.0 | nM | - |
| CHEMBL237788 | — | Activity | - | — | - |