Assay Detail
Binding
CHEMBL4840464
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human TRKA (436 to 790 residues) expressed in baculovirus infected Sf21 cells using TK as substrate in presence of ATP measured after 30 mins by HTRF assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.46 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4856292 | — | — | 1 | 8.47 |
| CHEMBL4862017 | — | — | 1 | 7.85 |
| CHEMBL4849505 | — | — | 1 | 7.77 |
| CHEMBL4856835 | — | — | 1 | 7.77 |
| CHEMBL4866306 | — | — | 1 | 7.54 |
| CHEMBL4867878 | — | — | 1 | 7.16 |
| CHEMBL4858842 | — | — | 1 | 7.02 |
| CHEMBL4870934 | — | — | 1 | 7.02 |
| CHEMBL4862580 | — | — | 1 | 6.92 |
| CHEMBL4858347 | — | — | 1 | 6.82 |
| CHEMBL4857029 | — | — | 1 | 6.75 |
| CHEMBL4853533 | — | — | 1 | 6.72 |
| CHEMBL4862417 | — | — | 1 | 6.70 |
| CHEMBL4846429 | — | — | 1 | 6.68 |
| CHEMBL4849227 | — | — | 1 | 6.68 |
| CHEMBL4858764 | — | — | 1 | 6.57 |
| CHEMBL4858605 | — | — | 1 | 6.57 |
| CHEMBL4870118 | — | — | 1 | 6.46 |
| CHEMBL4870710 | — | — | 1 | 6.38 |
| CHEMBL4877362 | — | — | 1 | 6.36 |
| CHEMBL4875527 | — | — | 1 | 6.35 |
| CHEMBL4867876 | — | — | 1 | 6.34 |
| CHEMBL4867883 | — | — | 1 | 6.33 |
| CHEMBL4868089 | — | — | 1 | 6.32 |
| CHEMBL4861545 | — | — | 1 | 6.28 |
| CHEMBL4857059 | — | — | 1 | 6.22 |
| CHEMBL4876967 | — | — | 1 | 6.17 |
| CHEMBL4877848 | — | — | 1 | 6.17 |
| CHEMBL4860060 | — | — | 1 | 6.15 |
| CHEMBL4874520 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4856292 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4862017 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4856835 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4849505 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4866306 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4867878 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4858842 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4870934 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4862580 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4858347 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4857029 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4853533 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4862417 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4846429 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4849227 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4858764 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4858605 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4870118 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4870710 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4877362 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4875527 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4867876 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4867883 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4868089 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4861545 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4857059 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4876967 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4877848 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4860060 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4874520 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4872861 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4855305 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4876945 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4849791 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4856027 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4851895 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4852420 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4855712 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4874296 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL4870193 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL4869556 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4853956 | — | IC50 | = | 6960.0 | nM | 5.16 |
| CHEMBL4851397 | — | IC50 | = | 16360.0 | nM | 4.79 |