Assay Detail
Binding
CHEMBL5736877
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Probe Displacement Assay: The probe displacement assay is conducted as follows: In a 385 well plate, test compounds along with recombinantly expressed His-tagged protein corresponding to amino acids 575-869 of human Tyk2 (sequence shown below) at 2.5 nM, 40 nM ((R)N-(1-(3-(8-methyl-5-(methylamino)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridin-2-yl)phenyl)ethyl)-2-([3H]methylsulfonyl)benzamide) (preparation described below) and 80 μg/mL Copper His-Tag scintillation proximity assay beads (Perkin Elmer, Catalog #RPNQ0095) in 50 mM HEPES, pH 7.5, containing 100 μg/mL bovine serum albumin and 5% DMSO were incubated for 30 minutes at room temperature. The amount of radiolabeled probe (preparation described below) bound to Tyk2 was then quantified by scintillation counting, and the inhibition by the test compound calculated by comparison to wells either with no inhibitor (0% inhibition) or without Tyk2 (100% inhibition). The IC50 value is defined as the concentration of test compound required to inhibit radiolabeled probe binding by 50%.
111
Total Activities
35
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Amide-substituted heterocyclic compounds useful as modulators of IL-12, IL-23 and/or IFN alpha responses
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 8.04 | 9.06 |
| kon | 37 | - | - |
| k_off | 37 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5769986 | — | — | 3 | 9.06 |
| CHEMBL5811479 | — | — | 3 | 8.89 |
| CHEMBL5911713 | — | — | 3 | 8.84 |
| CHEMBL5951711 | — | — | 3 | 8.80 |
| CHEMBL5790327 | — | — | 6 | 8.78 |
| CHEMBL5964490 | — | — | 3 | 8.77 |
| CHEMBL5785364 | — | — | 3 | 8.76 |
| CHEMBL6061085 | — | — | 3 | 8.72 |
| CHEMBL5788866 | — | — | 3 | 8.71 |
| CHEMBL5943725 | — | — | 3 | 8.70 |
| CHEMBL5870323 | — | — | 3 | 8.29 |
| CHEMBL4596392 | CRAVACITINIB | 4.0 | 6 | 8.29 |
| CHEMBL5943664 | — | — | 3 | 8.28 |
| CHEMBL4804058 | — | — | 3 | 8.28 |
| CHEMBL5871904 | — | — | 3 | 8.25 |
| CHEMBL5944749 | — | — | 3 | 8.24 |
| CHEMBL4803460 | — | — | 3 | 8.21 |
| CHEMBL5880067 | — | — | 3 | 8.20 |
| CHEMBL4598367 | — | — | 3 | 8.18 |
| CHEMBL5750912 | — | — | 3 | 8.16 |
| CHEMBL5890970 | — | — | 3 | 8.16 |
| CHEMBL5994007 | — | — | 3 | 8.15 |
| CHEMBL5755510 | — | — | 3 | 8.14 |
| CHEMBL5877573 | — | — | 3 | 8.14 |
| CHEMBL6024760 | — | — | 3 | 8.13 |
| CHEMBL6057366 | — | — | 3 | 7.22 |
| CHEMBL5797338 | — | — | 3 | 7.16 |
| CHEMBL5951552 | — | — | 3 | 7.16 |
| CHEMBL6002978 | — | — | 3 | 7.16 |
| CHEMBL5805075 | — | — | 3 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5769986 | — | EC50 | = | 0.877 | nM | 9.06 |
| CHEMBL5811479 | — | EC50 | = | 1.28 | nM | 8.89 |
| CHEMBL5911713 | — | EC50 | = | 1.46 | nM | 8.84 |
| CHEMBL5951711 | — | EC50 | = | 1.59 | nM | 8.80 |
| CHEMBL5790327 | — | EC50 | = | 1.66 | nM | 8.78 |
| CHEMBL5964490 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5785364 | — | EC50 | = | 1.72 | nM | 8.76 |
| CHEMBL6061085 | — | EC50 | = | 1.89 | nM | 8.72 |
| CHEMBL5788866 | — | EC50 | = | 1.94 | nM | 8.71 |
| CHEMBL5943725 | — | EC50 | = | 2.02 | nM | 8.70 |
| CHEMBL5870323 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4596392 | CRAVACITINIB | EC50 | = | 5.13 | nM | 8.29 |
| CHEMBL4804058 | — | EC50 | = | 5.22 | nM | 8.28 |
| CHEMBL5943664 | — | EC50 | = | 5.21 | nM | 8.28 |
| CHEMBL5871904 | — | EC50 | = | 5.64 | nM | 8.25 |
| CHEMBL5944749 | — | EC50 | = | 5.72 | nM | 8.24 |
| CHEMBL4803460 | — | EC50 | = | 6.18 | nM | 8.21 |
| CHEMBL5790327 | — | EC50 | = | 6.17 | nM | 8.21 |
| CHEMBL5880067 | — | EC50 | = | 6.35 | nM | 8.20 |
| CHEMBL4596392 | CRAVACITINIB | EC50 | = | 6.53 | nM | 8.19 |
| CHEMBL4598367 | — | EC50 | = | 6.57 | nM | 8.18 |
| CHEMBL5890970 | — | EC50 | = | 6.97 | nM | 8.16 |
| CHEMBL5750912 | — | EC50 | = | 6.95 | nM | 8.16 |
| CHEMBL5994007 | — | EC50 | = | 7.13 | nM | 8.15 |
| CHEMBL5877573 | — | EC50 | = | 7.22 | nM | 8.14 |
| CHEMBL5755510 | — | EC50 | = | 7.19 | nM | 8.14 |
| CHEMBL6024760 | — | EC50 | = | 7.36 | nM | 8.13 |
| CHEMBL6057366 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5951552 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5797338 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL6002978 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5805075 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5980521 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5972586 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5945690 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5769100 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5789728 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL6002978 | — | kon | = | - | — | - |
| CHEMBL5870323 | — | kon | = | - | — | - |
| CHEMBL5964490 | — | k_off | = | - | s-1 | - |
| CHEMBL5964490 | — | kon | = | - | — | - |
| CHEMBL5870323 | — | k_off | = | - | s-1 | - |
| CHEMBL5750912 | — | k_off | = | - | s-1 | - |
| CHEMBL5750912 | — | kon | = | - | — | - |
| CHEMBL5805075 | — | kon | = | - | — | - |
| CHEMBL5951552 | — | k_off | = | - | s-1 | - |
| CHEMBL5951552 | — | kon | = | - | — | - |
| CHEMBL5871904 | — | k_off | = | - | s-1 | - |
| CHEMBL5944749 | — | kon | = | - | — | - |
| CHEMBL5805075 | — | k_off | = | - | s-1 | - |