Assay Detail
Functional
CHEMBL2060037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
45
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 45 | 6.62 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2057602 | — | — | 2 | 8.13 |
| CHEMBL2057618 | — | — | 1 | 7.89 |
| CHEMBL2057610 | — | — | 1 | 7.85 |
| CHEMBL2057614 | — | — | 2 | 7.79 |
| CHEMBL2057619 | — | — | 2 | 7.65 |
| CHEMBL2059221 | — | — | 1 | 7.56 |
| CHEMBL2059827 | — | — | 1 | 7.55 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 7.29 |
| CHEMBL2059821 | — | — | 1 | 7.09 |
| CHEMBL2057605 | — | — | 1 | 7.08 |
| CHEMBL2057603 | — | — | 1 | 6.85 |
| CHEMBL2057607 | — | — | 1 | 6.72 |
| CHEMBL2059224 | — | — | 1 | 6.65 |
| CHEMBL2059828 | — | — | 1 | 6.64 |
| CHEMBL2057620 | — | — | 1 | 6.56 |
| CHEMBL456145 | — | — | 1 | 6.54 |
| CHEMBL2057615 | — | — | 2 | 6.51 |
| CHEMBL2057606 | — | — | 1 | 6.07 |
| CHEMBL2057235 | — | — | 1 | 5.99 |
| CHEMBL2059226 | — | — | 1 | 5.95 |
| CHEMBL2057616 | — | — | 1 | 5.93 |
| CHEMBL2059825 | — | — | 1 | 5.89 |
| CHEMBL2059223 | — | — | 1 | 5.79 |
| CHEMBL2059222 | — | — | 1 | 5.75 |
| CHEMBL2059829 | — | — | 1 | 5.70 |
| CHEMBL2057604 | — | — | 1 | 5.61 |
| CHEMBL2059822 | — | — | 1 | 5.27 |
| CHEMBL2059225 | — | — | 1 | 5.26 |
| CHEMBL2057617 | — | — | 1 | 4.67 |
| CHEMBL2059824 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2057602 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2057618 | — | EC50 | = | 12.9 | nM | 7.89 |
| CHEMBL2057610 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2057614 | — | EC50 | = | 16.4 | nM | 7.79 |
| CHEMBL2057619 | — | EC50 | = | 22.5 | nM | 7.65 |
| CHEMBL2059221 | — | EC50 | = | 27.5 | nM | 7.56 |
| CHEMBL2059827 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2057614 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2057619 | — | EC50 | = | 43.4 | nM | 7.36 |
| CHEMBL573 | NIACIN | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2059821 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2057605 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2057602 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2057603 | — | EC50 | = | 141.0 | nM | 6.85 |
| CHEMBL2057607 | — | EC50 | = | 192.0 | nM | 6.72 |
| CHEMBL2059224 | — | EC50 | = | 225.0 | nM | 6.65 |
| CHEMBL2059828 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL2057620 | — | EC50 | = | 276.0 | nM | 6.56 |
| CHEMBL456145 | — | EC50 | = | 286.0 | nM | 6.54 |
| CHEMBL2057615 | — | EC50 | = | 311.0 | nM | 6.51 |
| CHEMBL2057615 | — | EC50 | = | 573.0 | nM | 6.24 |
| CHEMBL2057606 | — | EC50 | = | 857.0 | nM | 6.07 |
| CHEMBL2057235 | — | EC50 | = | 1024.0 | nM | 5.99 |
| CHEMBL2059226 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL2057616 | — | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL2059825 | — | EC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL2059223 | — | EC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL2059222 | — | EC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL2059829 | — | EC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL2057604 | — | EC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL2059822 | — | EC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL2059225 | — | EC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL2057617 | — | EC50 | = | 21280.0 | nM | 4.67 |
| CHEMBL2057927 | — | EC50 | - | — | - | |
| CHEMBL2057926 | — | EC50 | - | — | - | |
| CHEMBL2059227 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2059228 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2059823 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2059824 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2059826 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2057613 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2057612 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2057611 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2057609 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2057608 | — | EC50 | > | 10000.0 | nM | - |