Assay Detail
Binding
CHEMBL5738952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ADP-Glo Assay: Materials and Instruments Used in the ADP-Glo AssayVendor Cat No.Materials ACL Sino Biological 11769-H07BCoANa2 Sigma C3144Potassium Citrate Sigma 89306ATP Promega V915BADP-GloTM Kinase Assay Promega V9102kitHEPES Life Technologies 15630080MgCl2 Sigma M1028Brij 35 detergent Merck 203728DTT Sigma 646563DMSO MP 196055Optiplate-384, White 384- Perkin Elmer 6007290well384 dilution plate Corning 3657Topseal A Perkin Elmer E534196-well plate Nunc 249944InstrumentPlate reader Perkin Elmer Envision 2104Centrifuge Eppendorf 5810RCompounds of the present invention were evaluated in an ADP-GLO assay as follows:a) Dilute cpd 1:3 in succession in DMSO by hand for each cpds for 12 ptsb) Add 0.1 μL diluted cpd solution to assay plate, each dose with 2 replicatesc) Centrifuge 1000 RPM for 1 mind) Add 5 μL ACL working solution to 384-well assay plate, centrifuge 1000 RPM for 1 mine) Incubate at 25° C. for 15 minf) Add 5 μL substrate working solution to initiate reactiong) Final ACL reaction concentrations: 3 nM ACL, 15 μM ATP, 3 μM CoA, 300 μM Citrate, 0.01% Brij35, 4 mM DTT, 1% DMSO;h) Reference final conc: 30 uM starting Conc, 3× dilution, 11+0 points. Test cpd conc: 30/100 uM starting Conc, 3× dilution, 11+0 points.i) Incubate at 25° C. for 60 minj) Add 10 μL ADP Glo reagent, centrifuge 1000 RPM for 1 mink) Incubate at 25° C. for 40 minl) Add 20 μL kinase detection reagent, centrifuge 1000 RPM for 1 minm) Incubate at 25° C. for 40 minn) Read on Envision for US LUM as RLU
1431
Total Activities
474
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
ACLY inhibitors and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 477 | 5.26 | 6.56 |
| kon | 477 | - | - |
| k_off | 477 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5808222 | — | — | 3 | 6.56 |
| CHEMBL5863051 | — | — | 3 | 6.56 |
| CHEMBL5974091 | — | — | 3 | 6.56 |
| CHEMBL6001826 | — | — | 3 | 6.56 |
| CHEMBL5773846 | — | — | 3 | 6.56 |
| CHEMBL5958556 | — | — | 3 | 6.56 |
| CHEMBL5901159 | — | — | 3 | 6.56 |
| CHEMBL5798977 | — | — | 3 | 6.56 |
| CHEMBL6000371 | — | — | 3 | 6.56 |
| CHEMBL6040194 | — | — | 3 | 6.56 |
| CHEMBL5758375 | — | — | 3 | 6.56 |
| CHEMBL5954786 | — | — | 3 | 6.56 |
| CHEMBL5961584 | — | — | 3 | 6.56 |
| CHEMBL5845981 | — | — | 3 | 6.56 |
| CHEMBL6046481 | — | — | 3 | 6.56 |
| CHEMBL5822273 | — | — | 3 | 6.56 |
| CHEMBL5832161 | — | — | 3 | 6.56 |
| CHEMBL5740498 | — | — | 3 | 6.56 |
| CHEMBL5962452 | — | — | 3 | 6.56 |
| CHEMBL5965601 | — | — | 3 | 6.56 |
| CHEMBL5988531 | — | — | 3 | 6.56 |
| CHEMBL5954737 | — | — | 3 | 6.56 |
| CHEMBL5786824 | — | — | 3 | 6.56 |
| CHEMBL5817088 | — | — | 3 | 6.56 |
| CHEMBL5784569 | — | — | 3 | 6.56 |
| CHEMBL5763642 | — | — | 3 | 6.56 |
| CHEMBL5962773 | — | — | 3 | 6.56 |
| CHEMBL5751874 | — | — | 3 | 6.56 |
| CHEMBL5901776 | — | — | 3 | 6.56 |
| CHEMBL6034869 | — | — | 3 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6046420 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5918706 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6001826 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5892768 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5873494 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6060515 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5773846 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5961584 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5954786 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6015133 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5969689 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5740498 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5767000 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6000371 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5962452 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6007053 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6034869 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5817088 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5758375 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5958556 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5962098 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5988531 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5808222 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6040194 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5892723 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6060170 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6062246 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5787145 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5822273 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5784569 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5999264 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5763642 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5832161 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5962773 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5894783 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5863051 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5751874 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5873469 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5786824 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5767187 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5954737 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5971206 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5933178 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5886047 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5901159 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5938509 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5974091 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5798977 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5923465 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL6037631 | — | IC50 | = | 275.0 | nM | 6.56 |