Assay Detail
Binding
CHEMBL5737465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity Assays: Measurement of forskolin stimulated inhibition of cAMP was performed via time-resolved fluorescence resonance energy transfer (TR-FRET) LANCE assay (AD0262, PerkinElmer Life Science, Inc., Boston Mass.). Recombinant Chinese hamster ovary (CHO-K1) cells expressing human somatostatin SSTR4 cells (ES-524-CF, PerkinElmer Life Science, Inc., Boston Mass.) were thawed (37° C.), resuspended in 10 mL Hanks' balanced salt solution no phenol red (HBSS, Invitrogen, Carlsbad Calif.), and then centrifuged (150×g, 5 minutes). Cellular pellet resuspended in stimulation buffer containing HBSS 1×, HEPES 5 mM, Protease free BSA 0.1% (PerkinElmer), and 3-Isobutyl-1-methylxanthine 0.5 mM (pH 7.4) and seeded in 96-well plates at 4000 cells/well. LANCE cAMP assay was performed per manufacture instruction with assessment of respective compound, somatostatin-28 (Sigma-Aldrich Co., St. Louis, Mo.) as control agonist, against 5 μM forskolin, performed in triplicate across concentration curve. Fluorescence signal was measured at 20 hours (excitation 340 nm and emission 665 nm, 400-μs delay) via TR-FRET (FLUOSTAR Omega-F, BMG Labtech, Inc., Cary, N.C.). Data was calculated via GraphPad PRISM-5 software.
198
Total Activities
66
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 66 | 7.64 | 9.60 |
| kon | 66 | - | - |
| k_off | 66 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193727 | — | — | 3 | 9.60 |
| CHEMBL5190457 | — | — | 3 | 9.56 |
| CHEMBL5177487 | — | — | 3 | 9.23 |
| CHEMBL6025625 | — | — | 3 | 9.21 |
| CHEMBL5175637 | — | — | 3 | 9.14 |
| CHEMBL5815501 | — | — | 3 | 9.00 |
| CHEMBL5206148 | — | — | 3 | 9.00 |
| CHEMBL5180551 | — | — | 3 | 8.89 |
| CHEMBL5188841 | — | — | 3 | 8.75 |
| CHEMBL5208396 | — | — | 3 | 8.69 |
| CHEMBL5196971 | — | — | 3 | 8.55 |
| CHEMBL5793940 | — | — | 3 | 8.51 |
| CHEMBL5177573 | — | — | 3 | 8.50 |
| CHEMBL5171935 | — | — | 3 | 8.48 |
| CHEMBL5189042 | — | — | 3 | 8.36 |
| CHEMBL5198142 | — | — | 3 | 8.25 |
| CHEMBL5195145 | — | — | 3 | 8.22 |
| CHEMBL5178013 | — | — | 3 | 8.22 |
| CHEMBL5200786 | — | — | 3 | 8.22 |
| CHEMBL5193686 | — | — | 3 | 8.18 |
| CHEMBL5205904 | — | — | 3 | 8.14 |
| CHEMBL5193172 | — | — | 3 | 8.14 |
| CHEMBL5800205 | — | — | 3 | 8.07 |
| CHEMBL5188361 | — | — | 3 | 8.05 |
| CHEMBL6032205 | — | — | 3 | 8.00 |
| CHEMBL5179321 | — | — | 3 | 7.97 |
| CHEMBL5991254 | — | — | 3 | 7.85 |
| CHEMBL5207543 | — | — | 3 | 7.81 |
| CHEMBL5201594 | — | — | 3 | 7.78 |
| CHEMBL5202717 | — | — | 3 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193727 | — | EC50 | = | 0.249 | nM | 9.60 |
| CHEMBL5190457 | — | EC50 | = | 0.276 | nM | 9.56 |
| CHEMBL5177487 | — | EC50 | = | 0.585 | nM | 9.23 |
| CHEMBL6025625 | — | EC50 | = | 0.619 | nM | 9.21 |
| CHEMBL5175637 | — | EC50 | = | 0.725 | nM | 9.14 |
| CHEMBL5815501 | — | EC50 | = | 0.992 | nM | 9.00 |
| CHEMBL5206148 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5180551 | — | EC50 | = | 1.28 | nM | 8.89 |
| CHEMBL5188841 | — | EC50 | = | 1.76 | nM | 8.75 |
| CHEMBL5208396 | — | EC50 | = | 2.03 | nM | 8.69 |
| CHEMBL5196971 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5793940 | — | EC50 | = | 3.09 | nM | 8.51 |
| CHEMBL5177573 | — | EC50 | = | 3.17 | nM | 8.50 |
| CHEMBL5171935 | — | EC50 | = | 3.32 | nM | 8.48 |
| CHEMBL5189042 | — | EC50 | = | 4.35 | nM | 8.36 |
| CHEMBL5198142 | — | EC50 | = | 5.63 | nM | 8.25 |
| CHEMBL5200786 | — | EC50 | = | 6.08 | nM | 8.22 |
| CHEMBL5195145 | — | EC50 | = | 6.02 | nM | 8.22 |
| CHEMBL5178013 | — | EC50 | = | 5.97 | nM | 8.22 |
| CHEMBL5193686 | — | EC50 | = | 6.65 | nM | 8.18 |
| CHEMBL5205904 | — | EC50 | = | 7.26 | nM | 8.14 |
| CHEMBL5193172 | — | EC50 | = | 7.27 | nM | 8.14 |
| CHEMBL5800205 | — | EC50 | = | 8.41 | nM | 8.07 |
| CHEMBL5188361 | — | EC50 | = | 8.81 | nM | 8.05 |
| CHEMBL6032205 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5179321 | — | EC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5991254 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5207543 | — | EC50 | = | 15.6 | nM | 7.81 |
| CHEMBL5201594 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5202717 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5890238 | — | EC50 | = | 17.5 | nM | 7.76 |
| CHEMBL5191532 | — | EC50 | = | 17.3 | nM | 7.76 |
| CHEMBL5193951 | — | EC50 | = | 19.3 | nM | 7.71 |
| CHEMBL5209165 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5176020 | — | EC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5839328 | — | EC50 | = | 21.9 | nM | 7.66 |
| CHEMBL5200112 | — | EC50 | = | 22.7 | nM | 7.64 |
| CHEMBL6027254 | — | EC50 | = | 25.2 | nM | 7.60 |
| CHEMBL5203972 | — | EC50 | = | 28.9 | nM | 7.54 |
| CHEMBL5981396 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL6006996 | — | EC50 | = | 38.5 | nM | 7.42 |
| CHEMBL5971636 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5968049 | — | EC50 | = | 46.9 | nM | 7.33 |
| CHEMBL5850435 | — | EC50 | = | 52.8 | nM | 7.28 |
| CHEMBL5192791 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5201540 | — | EC50 | = | 75.8 | nM | 7.12 |
| CHEMBL5180116 | — | EC50 | = | 77.7 | nM | 7.11 |
| CHEMBL5948967 | — | EC50 | = | 85.2 | nM | 7.07 |
| CHEMBL5769567 | — | EC50 | = | 89.3 | nM | 7.05 |
| CHEMBL5197218 | — | EC50 | = | 98.4 | nM | 7.01 |