Assay Detail
Binding
CHEMBL4308448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged recombinant human ATP-activated TRKA kinase domain (441 to 796 residues) expressed in baculovirus expression system preincubated with enzyme/ATP mixture for 20 mins followed by TK substrate-biotin addition followed by further incubation for 15 mins in presence of ATP by HTRF assay
120
Total Activities
120
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 |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Lead identification and characterization of hTrkA type 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 120 | 6.60 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4444901 | — | — | 1 | 8.66 |
| CHEMBL4577285 | — | — | 1 | 8.42 |
| CHEMBL4573890 | — | — | 1 | 8.17 |
| CHEMBL4524989 | — | — | 1 | 8.11 |
| CHEMBL4461600 | — | — | 1 | 8.10 |
| CHEMBL4466061 | — | — | 1 | 8.04 |
| CHEMBL4458913 | — | — | 1 | 7.99 |
| CHEMBL4553953 | — | — | 1 | 7.94 |
| CHEMBL4468419 | — | — | 1 | 7.92 |
| CHEMBL4545062 | — | — | 1 | 7.73 |
| CHEMBL4515321 | — | — | 1 | 7.71 |
| CHEMBL4448181 | — | — | 1 | 7.70 |
| CHEMBL4467890 | — | — | 1 | 7.68 |
| CHEMBL4557960 | — | — | 1 | 7.62 |
| CHEMBL4527557 | — | — | 1 | 7.61 |
| CHEMBL4592814 | — | — | 1 | 7.61 |
| CHEMBL4545212 | — | — | 1 | 7.61 |
| CHEMBL4466950 | — | — | 1 | 7.59 |
| CHEMBL4590914 | — | — | 1 | 7.58 |
| CHEMBL4456764 | — | — | 1 | 7.55 |
| CHEMBL4563845 | — | — | 1 | 7.51 |
| CHEMBL4439123 | — | — | 1 | 7.49 |
| CHEMBL4443873 | — | — | 1 | 7.49 |
| CHEMBL4458775 | — | — | 1 | 7.42 |
| CHEMBL4533532 | — | — | 1 | 7.38 |
| CHEMBL4450785 | — | — | 1 | 7.38 |
| CHEMBL4579043 | — | — | 1 | 7.38 |
| CHEMBL4461532 | — | — | 1 | 7.35 |
| CHEMBL4470140 | — | — | 1 | 7.33 |
| CHEMBL4449741 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4444901 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4577285 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4573890 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4524989 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4461600 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4466061 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4458913 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4553953 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4468419 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4545062 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL4515321 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL4448181 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL4467890 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL4557960 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL4527557 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4545212 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4592814 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL4466950 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL4590914 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL4456764 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL4563845 | — | IC50 | = | 31.1 | nM | 7.51 |
| CHEMBL4443873 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL4439123 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL4458775 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL4579043 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL4533532 | — | IC50 | = | 41.5 | nM | 7.38 |
| CHEMBL4450785 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL4461532 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL4470140 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL4449741 | — | IC50 | = | 51.1 | nM | 7.29 |
| CHEMBL4536149 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4561854 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL4451361 | — | IC50 | = | 59.1 | nM | 7.23 |
| CHEMBL4466913 | — | IC50 | = | 60.3 | nM | 7.22 |
| CHEMBL4562063 | — | IC50 | = | 62.3 | nM | 7.21 |
| CHEMBL4552667 | — | IC50 | = | 65.4 | nM | 7.18 |
| CHEMBL4452210 | — | IC50 | = | 65.9 | nM | 7.18 |
| CHEMBL4546610 | — | IC50 | = | 67.6 | nM | 7.17 |
| CHEMBL4453384 | — | IC50 | = | 67.5 | nM | 7.17 |
| CHEMBL4584518 | — | IC50 | = | 69.3 | nM | 7.16 |
| CHEMBL4463148 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4547987 | — | IC50 | = | 83.1 | nM | 7.08 |
| CHEMBL4461469 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4458705 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4579460 | — | IC50 | = | 107.4 | nM | 6.97 |
| CHEMBL4518353 | — | IC50 | = | 112.5 | nM | 6.95 |
| CHEMBL4439176 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4520451 | — | IC50 | = | 127.7 | nM | 6.89 |
| CHEMBL4451409 | — | IC50 | = | 128.7 | nM | 6.89 |
| CHEMBL4518910 | — | IC50 | = | 135.9 | nM | 6.87 |