Assay Detail
Binding
CHEMBL923137
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Inhibition of murine Lck by TR-FRET assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Proto-oncogene tyrosine-protein kinase LCK (CHEMBL2480) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.37 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249317 | — | — | 1 | 8.07 |
| CHEMBL398422 | — | — | 1 | 7.92 |
| CHEMBL249097 | — | — | 1 | 7.89 |
| CHEMBL248676 | — | — | 1 | 7.72 |
| CHEMBL398894 | — | — | 1 | 7.48 |
| CHEMBL250324 | — | — | 1 | 7.40 |
| CHEMBL250323 | — | — | 1 | 7.39 |
| CHEMBL399381 | — | — | 1 | 7.27 |
| CHEMBL251759 | — | — | 1 | 7.26 |
| CHEMBL399954 | — | — | 1 | 7.14 |
| CHEMBL249917 | — | — | 1 | 7.07 |
| CHEMBL400798 | — | — | 1 | 7.05 |
| CHEMBL249918 | — | — | 1 | 7.01 |
| CHEMBL251549 | GW782612X | — | 1 | 7.00 |
| CHEMBL249713 | — | — | 1 | 7.00 |
| CHEMBL249098 | — | — | 1 | 6.89 |
| CHEMBL250322 | — | — | 1 | 6.72 |
| CHEMBL249916 | — | — | 1 | 6.57 |
| CHEMBL249318 | — | — | 1 | 6.46 |
| CHEMBL399064 | — | — | 1 | 6.42 |
| CHEMBL443240 | — | — | 1 | 6.31 |
| CHEMBL251758 | — | — | 1 | 6.28 |
| CHEMBL250543 | — | — | 1 | 6.25 |
| CHEMBL399955 | — | — | 1 | 6.06 |
| CHEMBL249316 | — | — | 1 | 5.96 |
| CHEMBL400499 | — | — | 1 | 5.89 |
| CHEMBL398421 | — | — | 1 | 5.85 |
| CHEMBL250902 | — | — | 1 | 5.80 |
| CHEMBL248898 | — | — | 1 | 5.75 |
| CHEMBL250340 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249317 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL398422 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL249097 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL248676 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL398894 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL250324 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL250323 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL399381 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL251759 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL399954 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL249917 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL400798 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL249918 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL251549 | GW782612X | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL249713 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL249098 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL250322 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL249916 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL249318 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL399064 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL443240 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL251758 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL250543 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL399955 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL249316 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL400499 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL398421 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL250902 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL248898 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL250340 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL248897 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL251096 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL399382 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL398886 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL400388 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL430201 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL250542 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL251548 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL248707 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL400320 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL248706 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL249514 | — | IC50 | = | 16000.0 | nM | 4.80 |