Assay Detail
Binding
CHEMBL3706338
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated, and injected into mouse lymphoid cell line BA/F3 cells. Using a magnetic bead reagent for cell separation and a purification column (anti-CD8 monoclonal antibody immobilized on magnetic beads and a MiniMACS purification column; both are products of MilteDyi Biotec Inc.), cell surface CD8-expressing cells were purified to establish EML4-ALK fusion protein v1-expressing BA/F3 cells. From the cells, EML4-ALK fusion protein v1 was purified and subjected to kinase activity evaluation. EML4-ALK fusion protein v1 was investigated for its phosphorylation activity toward a peptide substrate by using a kinase activity detection kit (HTRF KinEASE-TK; Cisbio Inc.). Test compounds were each added to a reaction solution containing the enzyme protein to give 8 final concentrations from 1000 nM to 0.3 nM, followed by addition of ATP.
41
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | lymphoid |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Diamino heterocyclic carboxamide compound
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 8.82 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3687205 | — | — | 1 | 9.77 |
| CHEMBL3687207 | — | — | 1 | 9.68 |
| CHEMBL3687206 | — | — | 1 | 9.66 |
| CHEMBL3889838 | — | — | 1 | 9.64 |
| CHEMBL3687201 | — | — | 1 | 9.62 |
| CHEMBL3687204 | — | — | 1 | 9.59 |
| CHEMBL3687211 | — | — | 1 | 9.59 |
| CHEMBL3687202 | — | — | 1 | 9.59 |
| CHEMBL3687198 | — | — | 1 | 9.48 |
| CHEMBL3687209 | — | — | 1 | 9.47 |
| CHEMBL3687193 | — | — | 1 | 9.43 |
| CHEMBL3687210 | — | — | 1 | 9.31 |
| CHEMBL3687200 | — | — | 1 | 9.19 |
| CHEMBL3687197 | — | — | 1 | 9.11 |
| CHEMBL3687212 | — | — | 1 | 9.03 |
| CHEMBL3687208 | — | — | 1 | 9.03 |
| CHEMBL3687189 | — | — | 1 | 9.00 |
| CHEMBL3687216 | — | — | 1 | 9.00 |
| CHEMBL3687223 | — | — | 1 | 8.85 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 8.82 |
| CHEMBL3687215 | — | — | 1 | 8.82 |
| CHEMBL3975354 | — | — | 1 | 8.77 |
| CHEMBL3687218 | — | — | 1 | 8.72 |
| CHEMBL3687195 | — | — | 1 | 8.68 |
| CHEMBL3687221 | — | — | 1 | 8.68 |
| CHEMBL3687225 | — | — | 1 | 8.66 |
| CHEMBL3687217 | — | — | 1 | 8.64 |
| CHEMBL3687214 | — | — | 2 | 8.59 |
| CHEMBL3687213 | — | — | 2 | 8.55 |
| CHEMBL3687194 | — | — | 1 | 8.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3687205 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3687207 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL3687206 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3889838 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3687201 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3687204 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3687211 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3687202 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3687198 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3687209 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3687193 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL3687210 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3687200 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL3687197 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL3687208 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL3687212 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL3687189 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL3687216 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3687223 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3687215 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3301622 | GILTERITINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3975354 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3687218 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3687221 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3687195 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3687225 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3687217 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3687214 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3687194 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3687213 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3687213 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3687214 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3687224 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3687191 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3687220 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3687190 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3687219 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3687222 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3687188 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3687199 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3687192 | — | IC50 | = | 76.0 | nM | 7.12 |