Assay Detail
Binding
CHEMBL3705264
Review assay metadata, readout intent, target linkage, and publication context from the same page.
AlphaScreen Assay: Compounds of the invention were tested for ACK1 inhibition activity. 1 uL compounds prepared at 15× in 4 mM DMSO were combined with 9 uL ATP solution in assay buffer containing 50 mM Hepes, 1% glycerol, 1.665 mM MnCl2 and Poly-(GT)-Biotin (Cisbio #61GT0BLD, 1:1500 dilution) in ProxiPlate-384 Plus plate (PerkinElmer #6008280). Final DMSO concentration was 0.25% with an ATP final concentration of 100 uM. The reaction was started by adding 5 uL ACK1 solution (Carna, 15 pg/uL final in assay) in an enzyme buffer containing 50 mM Hepes, 0.24 mM EGTA, 0.024% Brij-35, 3 mM DTT, 0.01% BSA. Reaction was allowed to occur for 20 min., shaking, at RT. Anti PT66 acceptor beads and Streptavidin donor beads (PerkinElmer #6760602R) were prepared by adding each at 1:160 dilution in a detection buffer containing 25 mM Tris-HCl, 250 mM NaCl, 100 mM EDTA, 0.25% BSA. Prepared beads were added to assay plate at 5 uL well and allowed to incubate protected from light, shaking, for 2 hrs at RT. Plates were read on AlphaQuest reader.
348
Total Activities
346
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted imidazopyr- and imidazotri-azines
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 348 | 6.00 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3655208 | — | — | 1 | 7.52 |
| CHEMBL3651341 | — | — | 1 | 7.45 |
| CHEMBL3655246 | — | — | 1 | 7.43 |
| CHEMBL3655151 | — | — | 1 | 7.36 |
| CHEMBL2325971 | — | — | 1 | 7.31 |
| CHEMBL3651315 | — | — | 1 | 7.30 |
| CHEMBL3655247 | — | — | 1 | 7.30 |
| CHEMBL3651376 | — | — | 1 | 7.23 |
| CHEMBL3651342 | — | — | 1 | 7.22 |
| CHEMBL3655153 | — | — | 1 | 7.18 |
| CHEMBL2325947 | — | — | 1 | 7.12 |
| CHEMBL3655223 | — | — | 1 | 7.12 |
| CHEMBL2325972 | — | — | 1 | 7.06 |
| CHEMBL2325952 | — | — | 1 | 7.06 |
| CHEMBL2325960 | — | — | 1 | 7.05 |
| CHEMBL2325954 | — | — | 1 | 7.05 |
| CHEMBL3651310 | — | — | 1 | 7.02 |
| CHEMBL2325961 | — | — | 1 | 7.02 |
| CHEMBL3651363 | — | — | 1 | 7.00 |
| CHEMBL2325964 | — | — | 1 | 6.96 |
| CHEMBL3655243 | — | — | 1 | 6.96 |
| CHEMBL3655237 | — | — | 1 | 6.95 |
| CHEMBL3651380 | — | — | 1 | 6.94 |
| CHEMBL2325959 | — | — | 1 | 6.93 |
| CHEMBL2325940 | — | — | 1 | 6.92 |
| CHEMBL3655156 | — | — | 1 | 6.92 |
| CHEMBL3655269 | — | — | 1 | 6.87 |
| CHEMBL2325958 | — | — | 1 | 6.86 |
| CHEMBL2325939 | — | — | 1 | 6.86 |
| CHEMBL3655225 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3655208 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3651341 | — | IC50 | = | 35.2 | nM | 7.45 |
| CHEMBL3655246 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL3655151 | — | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL2325971 | — | IC50 | = | 48.7 | nM | 7.31 |
| CHEMBL3651315 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3655247 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3651376 | — | IC50 | = | 58.9 | nM | 7.23 |
| CHEMBL3651342 | — | IC50 | = | 60.4 | nM | 7.22 |
| CHEMBL3655153 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL3655223 | — | IC50 | = | 75.1 | nM | 7.12 |
| CHEMBL2325947 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2325952 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL2325972 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2325960 | — | IC50 | = | 88.6 | nM | 7.05 |
| CHEMBL2325954 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3651310 | — | IC50 | = | 95.8 | nM | 7.02 |
| CHEMBL2325961 | — | IC50 | = | 95.2 | nM | 7.02 |
| CHEMBL3651363 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3655243 | — | IC50 | = | 109.8 | nM | 6.96 |
| CHEMBL2325964 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL3655237 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3651380 | — | IC50 | = | 114.6 | nM | 6.94 |
| CHEMBL2325959 | — | IC50 | = | 116.8 | nM | 6.93 |
| CHEMBL2325940 | — | IC50 | = | 118.8 | nM | 6.92 |
| CHEMBL3655156 | — | IC50 | = | 121.7 | nM | 6.92 |
| CHEMBL3655269 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL3655225 | — | IC50 | = | 138.7 | nM | 6.86 |
| CHEMBL2325939 | — | IC50 | = | 137.1 | nM | 6.86 |
| CHEMBL2325958 | — | IC50 | = | 139.6 | nM | 6.86 |
| CHEMBL3655146 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL245408 | — | IC50 | = | 147.8 | nM | 6.83 |
| CHEMBL3651314 | — | IC50 | = | 152.6 | nM | 6.82 |
| CHEMBL3655221 | — | IC50 | = | 153.6 | nM | 6.81 |
| CHEMBL3655254 | — | IC50 | = | 175.9 | nM | 6.75 |
| CHEMBL3651379 | — | IC50 | = | 178.2 | nM | 6.75 |
| CHEMBL3651377 | — | IC50 | = | 183.2 | nM | 6.74 |
| CHEMBL3651340 | — | IC50 | = | 181.3 | nM | 6.74 |
| CHEMBL3651361 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3655139 | — | IC50 | = | 183.4 | nM | 6.74 |
| CHEMBL3655160 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL3651357 | — | IC50 | = | 188.3 | nM | 6.72 |
| CHEMBL3655260 | — | IC50 | = | 196.7 | nM | 6.71 |
| CHEMBL3655255 | — | IC50 | = | 199.1 | nM | 6.70 |
| CHEMBL3655259 | — | IC50 | = | 201.4 | nM | 6.70 |
| CHEMBL3651359 | — | IC50 | = | 203.1 | nM | 6.69 |
| CHEMBL3651339 | — | IC50 | = | 205.3 | nM | 6.69 |
| CHEMBL3655256 | — | IC50 | = | 216.4 | nM | 6.67 |
| CHEMBL2325938 | — | IC50 | = | 216.1 | nM | 6.67 |
| CHEMBL3651307 | — | IC50 | = | 212.0 | nM | 6.67 |