Assay Detail
Binding
CHEMBL3887041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Amplified Luminescent Proximity Assay: To measure JAK2 kinase activity, a commercially available purified enzyme may be used. The enzyme may be a C-terminal His6-tagged, recombinant, human JAK2, amino acids 808-end, (Genbank Accession number NM 004972) expressed by baculovirus in Sf21 cells (Upstate Biotechnology MA). After incubation of the kinase with a biotinylated substrate and adenosine triphosphate (ATP) for 60 minutes at room temperature, the kinase reaction may be stopped by the addition of 30 mM ethylenediaminetetraacetic acid (EDTA). The reaction may be performed in 384 well microtitre plates and the reaction products may be detected with the addition of streptavidin coated Donor Beads and phosphotyrosine-specific antibodies coated Acceptor Beads using the EnVision Multilabel Plate Reader after an overnight incubation at room temperature.
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf21 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.75 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3639583 | — | — | 1 | 8.52 |
| CHEMBL2151323 | — | — | 2 | 8.52 |
| CHEMBL3659500 | — | — | 1 | 8.52 |
| CHEMBL3659499 | — | — | 1 | 8.52 |
| CHEMBL3659498 | — | — | 1 | 8.52 |
| CHEMBL2151322 | — | — | 1 | 8.52 |
| CHEMBL3659497 | AZD-7451 | 1.0 | 1 | 8.52 |
| CHEMBL2151319 | — | — | 1 | 8.52 |
| CHEMBL2151321 | — | — | 1 | 8.52 |
| CHEMBL3659494 | — | — | 1 | 8.52 |
| CHEMBL3659502 | — | — | 1 | 8.40 |
| CHEMBL3659496 | — | — | 1 | 8.30 |
| CHEMBL3659501 | — | — | 1 | 8.22 |
| CHEMBL3659495 | — | — | 1 | 7.92 |
| CHEMBL3659504 | — | — | 1 | 7.85 |
| CHEMBL2151320 | — | — | 1 | 7.21 |
| CHEMBL3659508 | — | — | 1 | 7.02 |
| CHEMBL3659505 | — | — | 1 | 6.51 |
| CHEMBL3659507 | — | — | 1 | 6.32 |
| CHEMBL3659509 | — | — | 1 | 6.11 |
| CHEMBL3659503 | — | — | 1 | 5.42 |
| CHEMBL3659506 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3639583 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2151321 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2151323 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659500 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659499 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659498 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2151322 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659497 | AZD-7451 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2151319 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659494 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2151323 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3659502 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3659496 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3659501 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3659495 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3659504 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2151320 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3659508 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3659505 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL3659507 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL3659509 | — | IC50 | = | 773.0 | nM | 6.11 |
| CHEMBL3659503 | — | IC50 | = | 3809.0 | nM | 5.42 |
| CHEMBL3659506 | — | IC50 | = | 7250.0 | nM | 5.14 |