Assay Detail
Binding
CHEMBL5732865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
CDK8/Cyclin C Binding Assay: The binding assay relies on the LanthaScreen Eu-Kinase Binding Assay (Invitrogen. This is a kinase assay platform based on measuring the binding and displacement of an Alexa Fluor® 647 conjugate of an ATP-competitive kinase inhibitor (Kinase Tracer 236, PV5592) at a kinase active site. Binding of the tracer to the kinase is detected by addition of a europium (Eu)-labelled anti-His antibody (Invitrogen PV 5596), which specifically labels the kinase of interest. This binding results in a high degree of fluorescence resonance energy transfer (FRET), whereas displacement of the tracer with a kinase inhibitor results in a loss of FRET.The enzyme has been purchase from Invitrogen (PV4402) as a dimer of full-length His-tagged recombinant human proteins.Assay conditions were as indicated by the kit manufacturers with the following adaptations:Assay buffer: 50 mM HEPES, pH 7.5, 1 mM EGTA, 0.01% Brij-35, 10 mM MgCl2Assay volume: 25 μlIncubation time and temperature: 60 min at 25° C.Cdk8-Cyclin C concentration: 5 nMTracer concentration: 10 nM(Eu)-labeled anti-His antibody concentration: 1.5 nMTested compound: Serial 1:3 dilutionsFinal DMSO concentration in the assay: 1%Assays were performed in 384-well plates. The final read out was generated using an EnVision plate reader (Perkin-Elmer). The emission ratio was calculated by dividing the acceptor/tracer emission (665 nm) by the antibody/donor emission (615 nm).
291
Total Activities
97
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Condensed tricyclic compounds as protein kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 97 | 7.26 | 9.72 |
| kon | 97 | - | - |
| k_off | 97 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789125 | — | — | 3 | 9.72 |
| CHEMBL4789603 | — | — | 3 | 9.58 |
| CHEMBL4776812 | — | — | 3 | 9.56 |
| CHEMBL4777356 | — | — | 3 | 9.50 |
| CHEMBL5752178 | — | — | 3 | 9.39 |
| CHEMBL4780792 | — | — | 3 | 9.33 |
| CHEMBL4782696 | — | — | 3 | 8.96 |
| CHEMBL5817322 | — | — | 3 | 8.87 |
| CHEMBL4779550 | — | — | 3 | 8.85 |
| CHEMBL4791276 | — | — | 3 | 8.85 |
| CHEMBL4778840 | — | — | 3 | 8.85 |
| CHEMBL4778755 | — | — | 3 | 8.85 |
| CHEMBL4785713 | — | — | 3 | 8.71 |
| CHEMBL4797707 | — | — | 3 | 8.70 |
| CHEMBL4789863 | — | — | 3 | 8.68 |
| CHEMBL4781993 | — | — | 3 | 8.66 |
| CHEMBL4793447 | — | — | 3 | 8.62 |
| CHEMBL4782944 | — | — | 3 | 8.59 |
| CHEMBL4797007 | — | — | 3 | 8.58 |
| CHEMBL4790936 | — | — | 3 | 8.49 |
| CHEMBL4794862 | — | — | 3 | 8.42 |
| CHEMBL5943185 | — | — | 3 | 8.38 |
| CHEMBL4792305 | — | — | 3 | 8.36 |
| CHEMBL5767742 | — | — | 3 | 8.35 |
| CHEMBL4795220 | — | — | 3 | 8.33 |
| CHEMBL4787064 | — | — | 3 | 8.13 |
| CHEMBL4777501 | — | — | 3 | 8.07 |
| CHEMBL5820678 | — | — | 3 | 8.05 |
| CHEMBL6022963 | — | — | 3 | 8.03 |
| CHEMBL6006771 | — | — | 3 | 7.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789125 | — | IC50 | = | 0.191 | nM | 9.72 |
| CHEMBL4789603 | — | IC50 | = | 0.262 | nM | 9.58 |
| CHEMBL4776812 | — | IC50 | = | 0.278 | nM | 9.56 |
| CHEMBL4777356 | — | IC50 | = | 0.314 | nM | 9.50 |
| CHEMBL5752178 | — | IC50 | = | 0.407 | nM | 9.39 |
| CHEMBL4780792 | — | IC50 | = | 0.466 | nM | 9.33 |
| CHEMBL4782696 | — | IC50 | = | 1.11 | nM | 8.96 |
| CHEMBL5817322 | — | IC50 | = | 1.36 | nM | 8.87 |
| CHEMBL4778755 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4778840 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4779550 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4791276 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4785713 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL4797707 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL4789863 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4781993 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL4793447 | — | IC50 | = | 2.41 | nM | 8.62 |
| CHEMBL4782944 | — | IC50 | = | 2.59 | nM | 8.59 |
| CHEMBL4797007 | — | IC50 | = | 2.65 | nM | 8.58 |
| CHEMBL4790936 | — | IC50 | = | 3.23 | nM | 8.49 |
| CHEMBL4794862 | — | IC50 | = | 3.83 | nM | 8.42 |
| CHEMBL5943185 | — | IC50 | = | 4.18 | nM | 8.38 |
| CHEMBL4792305 | — | IC50 | = | 4.33 | nM | 8.36 |
| CHEMBL5767742 | — | IC50 | = | 4.46 | nM | 8.35 |
| CHEMBL4795220 | — | IC50 | = | 4.64 | nM | 8.33 |
| CHEMBL4787064 | — | IC50 | = | 7.48 | nM | 8.13 |
| CHEMBL4777501 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5820678 | — | IC50 | = | 8.94 | nM | 8.05 |
| CHEMBL6022963 | — | IC50 | = | 9.32 | nM | 8.03 |
| CHEMBL6006771 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL6062128 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL4789450 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4792156 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL6002058 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4776992 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL5831525 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL4782056 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL5967061 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL6052876 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL5967245 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL5790753 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL6035709 | — | IC50 | = | 31.1 | nM | 7.51 |
| CHEMBL6017565 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL5755811 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL5975092 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL5770417 | — | IC50 | = | 54.7 | nM | 7.26 |
| CHEMBL5866937 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL4789204 | — | IC50 | = | 55.4 | nM | 7.26 |
| CHEMBL5748809 | — | IC50 | = | 61.1 | nM | 7.21 |
| CHEMBL6060510 | — | IC50 | = | 78.5 | nM | 7.11 |