Assay Detail
Binding
CHEMBL4052334
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human LOXL2 expressed in human whole blood assessed as reduction of H2O2 production from oxidative deamination of DAP preincubated for 2 hrs followed by substrate addition measured every 2 mins for 1 hr by amplex red reagent-based fluorescence assay
31
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.55 | 6.55 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082808 | — | — | 1 | 6.55 |
| CHEMBL4084982 | — | — | 1 | 6.51 |
| CHEMBL1618272 | — | — | 1 | 6.40 |
| CHEMBL4100783 | — | — | 1 | 6.26 |
| CHEMBL4097435 | — | — | 1 | 6.16 |
| CHEMBL4063337 | — | — | 1 | 6.15 |
| CHEMBL4105137 | — | — | 1 | 6.08 |
| CHEMBL4079398 | — | — | 2 | 6.06 |
| CHEMBL4071963 | — | — | 1 | 6.04 |
| CHEMBL4092740 | — | — | 1 | 5.94 |
| CHEMBL4088453 | — | — | 1 | 5.89 |
| CHEMBL4063420 | — | — | 1 | 5.85 |
| CHEMBL4067192 | — | — | 1 | 5.85 |
| CHEMBL4086010 | — | — | 1 | 5.80 |
| CHEMBL4093765 | — | — | 1 | 5.77 |
| CHEMBL4103928 | — | — | 1 | 5.75 |
| CHEMBL4087273 | — | — | 1 | 5.70 |
| CHEMBL4059919 | — | — | 1 | 5.54 |
| CHEMBL4078119 | — | — | 1 | 5.54 |
| CHEMBL4085053 | — | — | 1 | 5.28 |
| CHEMBL4063906 | — | — | 1 | 5.17 |
| CHEMBL4066637 | — | — | 1 | 5.10 |
| CHEMBL4066192 | — | — | 1 | 5.10 |
| CHEMBL4068580 | — | — | 1 | 5.00 |
| CHEMBL4089707 | — | — | 1 | 4.64 |
| CHEMBL4075255 | — | — | 1 | 4.54 |
| CHEMBL4085480 | — | — | 1 | 4.52 |
| CHEMBL4066086 | — | — | 1 | 4.46 |
| CHEMBL4096173 | — | — | 1 | 4.41 |
| CHEMBL4081837 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082808 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4084982 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1618272 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4100783 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4097435 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4063337 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4105137 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4079398 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4071963 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4092740 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4088453 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4067192 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4063420 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4086010 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4093765 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4103928 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4087273 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4078119 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4059919 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4085053 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4063906 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4066637 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4066192 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4068580 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4089707 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4075255 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL4085480 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4066086 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4096173 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4081837 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4079398 | — | IC90 | = | 5400.0 | nM | - |