Assay Detail
Functional
CHEMBL3365186
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Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
37
Total Activities
37
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
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 5.52 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415788 | — | — | 1 | 10.38 |
| CHEMBL462830 | — | — | 1 | 6.66 |
| CHEMBL3099773 | — | — | 1 | 6.53 |
| CHEMBL2431120 | — | — | 1 | 5.70 |
| CHEMBL3315193 | — | — | 1 | 5.69 |
| CHEMBL3315206 | — | — | 1 | 5.67 |
| CHEMBL3315222 | — | — | 1 | 5.54 |
| CHEMBL3315203 | — | — | 1 | 5.49 |
| CHEMBL3315199 | — | — | 1 | 5.49 |
| CHEMBL3315221 | — | — | 1 | 5.48 |
| CHEMBL3315213 | — | — | 1 | 5.36 |
| CHEMBL3315202 | — | — | 1 | 5.30 |
| CHEMBL3315209 | — | — | 1 | 5.29 |
| CHEMBL3315194 | — | — | 1 | 5.18 |
| CHEMBL3315223 | — | — | 1 | 5.13 |
| CHEMBL3315204 | — | — | 1 | 5.11 |
| CHEMBL463811 | — | — | 1 | 5.05 |
| CHEMBL3315200 | — | — | 1 | 5.03 |
| CHEMBL3315197 | — | — | 1 | 5.03 |
| CHEMBL3315195 | — | — | 1 | 5.00 |
| CHEMBL3315198 | — | — | 1 | 4.81 |
| CHEMBL3315205 | — | — | 1 | 4.62 |
| CHEMBL3315196 | — | — | 1 | 4.59 |
| CHEMBL3315201 | — | — | 1 | 4.26 |
| CHEMBL3315208 | — | — | 1 | - |
| CHEMBL3315210 | — | — | 1 | - |
| CHEMBL3315211 | — | — | 1 | - |
| CHEMBL3315212 | — | — | 1 | - |
| CHEMBL3315207 | — | — | 1 | - |
| CHEMBL3315214 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415788 | — | EC50 | = | 0.0416 | nM | 10.38 |
| CHEMBL462830 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3099773 | — | EC50 | = | 298.0 | nM | 6.53 |
| CHEMBL2431120 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3315193 | — | EC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL3315206 | — | EC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL3315222 | — | EC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL3315203 | — | EC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL3315199 | — | EC50 | = | 3260.0 | nM | 5.49 |
| CHEMBL3315221 | — | EC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL3315213 | — | EC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL3315202 | — | EC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL3315209 | — | EC50 | = | 5170.0 | nM | 5.29 |
| CHEMBL3315194 | — | EC50 | = | 6650.0 | nM | 5.18 |
| CHEMBL3315223 | — | EC50 | = | 7460.0 | nM | 5.13 |
| CHEMBL3315204 | — | EC50 | = | 7720.0 | nM | 5.11 |
| CHEMBL463811 | — | EC50 | = | 8990.0 | nM | 5.05 |
| CHEMBL3315197 | — | EC50 | = | 9440.0 | nM | 5.03 |
| CHEMBL3315200 | — | EC50 | = | 9390.0 | nM | 5.03 |
| CHEMBL3315195 | — | EC50 | = | 9990.0 | nM | 5.00 |
| CHEMBL3315198 | — | EC50 | = | 15380.0 | nM | 4.81 |
| CHEMBL3315205 | — | EC50 | = | 24200.0 | nM | 4.62 |
| CHEMBL3315196 | — | EC50 | = | 25820.0 | nM | 4.59 |
| CHEMBL3315201 | — | EC50 | = | 55070.0 | nM | 4.26 |
| CHEMBL496585 | — | EC50 | = | 178000.0 | nM | - |
| CHEMBL3315220 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315219 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315218 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315217 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315216 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315215 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315214 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315207 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315212 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315211 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315210 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3315208 | — | EC50 | > | 100000.0 | nM | - |