Assay Detail
Functional
CHEMBL924060
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Agonist lead identification for the high affinity niacin receptor GPR109a.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 41 | 5.43 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.92 |
| CHEMBL391574 | — | — | 1 | 6.34 |
| CHEMBL247134 | — | — | 1 | 6.30 |
| CHEMBL394498 | — | — | 1 | 6.10 |
| CHEMBL128604 | — | — | 1 | 6.07 |
| CHEMBL247098 | — | — | 1 | 6.00 |
| CHEMBL393428 | — | — | 1 | 5.89 |
| CHEMBL428730 | — | — | 1 | 5.85 |
| CHEMBL393226 | — | — | 1 | 5.82 |
| CHEMBL247921 | — | — | 1 | 5.75 |
| CHEMBL393086 | — | — | 1 | 5.68 |
| CHEMBL395177 | — | — | 1 | 5.66 |
| CHEMBL393085 | — | — | 1 | 5.60 |
| CHEMBL246903 | — | — | 1 | 5.60 |
| CHEMBL338071 | — | — | 1 | 5.57 |
| CHEMBL429495 | — | — | 1 | 5.55 |
| CHEMBL247316 | — | — | 1 | 5.54 |
| CHEMBL394885 | — | — | 1 | 5.43 |
| CHEMBL237788 | — | — | 1 | 5.41 |
| CHEMBL395118 | — | — | 1 | 5.31 |
| CHEMBL397783 | 5-FLUORONICOTINIC ACID | 3.0 | 1 | 5.28 |
| CHEMBL247724 | — | — | 1 | 5.25 |
| CHEMBL247922 | — | — | 1 | 5.25 |
| CHEMBL246692 | — | — | 1 | 5.21 |
| CHEMBL394441 | — | — | 1 | 5.21 |
| CHEMBL613 | PYRAZINOIC ACID | -1.0 | 1 | 5.20 |
| CHEMBL247526 | — | — | 1 | 5.18 |
| CHEMBL395178 | — | — | 1 | 5.12 |
| CHEMBL394688 | — | — | 1 | 5.08 |
| CHEMBL238002 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573 | NIACIN | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL391574 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL247134 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL394498 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL128604 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL247098 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL393428 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL428730 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL393226 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL247921 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL393086 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL395177 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL393085 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL246903 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL338071 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL429495 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL247316 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL394885 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL237788 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL395118 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL397783 | 5-FLUORONICOTINIC ACID | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL247922 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL247724 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL246692 | — | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL394441 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL613 | PYRAZINOIC ACID | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL247526 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL395178 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL394688 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL238002 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL245858 | — | EC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL247723 | — | EC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL247317 | — | EC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL255877 | — | EC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL247527 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL394464 | — | EC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL247336 | — | EC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL247132 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL245491 | — | EC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL394068 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL393429 | — | EC50 | > | 20000.0 | nM | - |