Assay Detail
Binding
CHEMBL3706359
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Scintillation Proximity Assay (SPA): The kinase assay is based on the LanthaScreen technology. LanthaScreen is the detection of Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) using lanthanide chelates to measure interactions between various binding partners. In a TR-FRET kinase assay, a long-lifetime lanthanide donor species is conjugated to an antibody that specifically binds to a phosphorylated product of a kinase reaction that is labeled with a suitable acceptor fluorophore. This antibody-mediated interaction brings the lanthanide donor and the acceptor into proximity such that resonance energy transfer can take place, resulting in a detectable increase in the FRET signal.The kinase reactions were performed in 384 well microtiter plates in a total reaction volume of 10.05 μL. The assay plates were prepared with 0.05 μL per well of test compound in the appropriate test concentration, as described under preparation of compound dilutions.
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Triazolopyridine compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 4.81 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 5.52 |
| CHEMBL3651404 | — | — | 1 | 5.40 |
| CHEMBL2133806 | JNJ-38877605 | 1.0 | 1 | 5.40 |
| CHEMBL3704015 | — | — | 1 | 5.22 |
| CHEMBL3703994 | — | — | 1 | 5.22 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 5.16 |
| CHEMBL3704020 | — | — | 1 | 5.16 |
| CHEMBL3703986 | — | — | 1 | 5.16 |
| CHEMBL3703992 | — | — | 1 | 5.00 |
| CHEMBL3704000 | — | — | 1 | 5.00 |
| CHEMBL3704013 | — | — | 1 | 4.96 |
| CHEMBL3704008 | — | — | 1 | 4.92 |
| CHEMBL3703996 | — | — | 1 | 4.92 |
| CHEMBL3703982 | — | — | 1 | 4.92 |
| CHEMBL3703989 | — | — | 1 | 4.89 |
| CHEMBL3703993 | — | — | 1 | 4.89 |
| CHEMBL3703940 | — | — | 1 | 4.85 |
| CHEMBL3704007 | — | — | 1 | 4.85 |
| CHEMBL3703988 | — | — | 1 | 4.85 |
| CHEMBL3703957 | — | — | 1 | 4.82 |
| CHEMBL3704018 | — | — | 1 | 4.82 |
| CHEMBL3703970 | — | — | 1 | 4.80 |
| CHEMBL3703961 | — | — | 1 | 4.77 |
| CHEMBL3703947 | — | — | 1 | 4.77 |
| CHEMBL3703991 | — | — | 1 | 4.77 |
| CHEMBL3703997 | — | — | 1 | 4.75 |
| CHEMBL3704005 | — | — | 1 | 4.75 |
| CHEMBL3703979 | — | — | 1 | 4.70 |
| CHEMBL3704014 | — | — | 1 | 4.70 |
| CHEMBL3703950 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1236107 | SGX-523 | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3651404 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2133806 | JNJ-38877605 | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3704015 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3703994 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2001019 | PF-04217903 | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3704020 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3703986 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3703992 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3704000 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3704013 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3704008 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3703996 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3703982 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3703993 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3703989 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3703940 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3704007 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3703988 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3703957 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3704018 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3703970 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3703961 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3703947 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3703991 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3703997 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3704005 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3703979 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3704014 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3703950 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3703964 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3703966 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3704017 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3704009 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3703978 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL3703945 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703965 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703968 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703981 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703985 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703958 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3704011 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703956 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3704016 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703952 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3703943 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3704010 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3704002 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3704001 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3704019 | — | IC50 | > | 30000.0 | nM | - |