Assay Detail
Binding
CHEMBL2350855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant truncated SYK (360 to 365 amino acid residues) using N-terminally biotinylated EPEGDYEEVLE peptide as substrate assessed as inhibition of [33P]-ATP incorporation incubated for 10 mins prior to substrate addition measured after 15 mins by scintillation counting
41
Total Activities
41
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 |
Publication
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.93 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2346686 | — | — | 1 | 9.00 |
| CHEMBL2177736 | — | — | 1 | 9.00 |
| CHEMBL2347405 | — | — | 1 | 8.70 |
| CHEMBL2347988 | — | — | 1 | 8.70 |
| CHEMBL2347418 | — | — | 1 | 8.52 |
| CHEMBL2347406 | — | — | 1 | 8.52 |
| CHEMBL2347420 | — | — | 1 | 8.52 |
| CHEMBL2348854 | — | — | 1 | 8.40 |
| CHEMBL2347413 | — | — | 1 | 8.40 |
| CHEMBL2347994 | — | — | 1 | 8.40 |
| CHEMBL2347417 | — | — | 1 | 8.40 |
| CHEMBL2347991 | — | — | 1 | 8.30 |
| CHEMBL2348858 | — | — | 1 | 8.30 |
| CHEMBL2347415 | — | — | 1 | 8.30 |
| CHEMBL2347989 | — | — | 1 | 8.30 |
| CHEMBL2348856 | — | — | 1 | 8.22 |
| CHEMBL2348853 | — | — | 1 | 8.15 |
| CHEMBL2177737 | — | — | 1 | 8.15 |
| CHEMBL2347414 | — | — | 1 | 8.00 |
| CHEMBL2347407 | — | — | 1 | 8.00 |
| CHEMBL2348855 | — | — | 1 | 7.89 |
| CHEMBL2348850 | — | — | 1 | 7.85 |
| CHEMBL2347990 | — | — | 1 | 7.80 |
| CHEMBL2347992 | — | — | 1 | 7.80 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 7.77 |
| CHEMBL2347416 | — | — | 1 | 7.72 |
| CHEMBL2347999 | — | — | 1 | 7.72 |
| CHEMBL2347998 | — | — | 1 | 7.62 |
| CHEMBL2347996 | — | — | 1 | 7.58 |
| CHEMBL2347419 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2346686 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2177736 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2347988 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2347405 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2347418 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2347406 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2347420 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2348854 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2347413 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2347994 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2347417 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2347991 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2347989 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2347415 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2348858 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2348856 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2348853 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2177737 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2347414 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2347407 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2348855 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2348850 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2347990 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2347992 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2103830 | FOSTAMATINIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2347416 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2347999 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2347998 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2347996 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2347419 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2347997 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2347409 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2348851 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2348852 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2348857 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2347410 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2347408 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2347412 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2347993 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2347995 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL2347411 | — | IC50 | = | 135.0 | nM | 6.87 |