Ready-To-Go Assays
Cutting-Edge & Cost-Efficient Services For Multiple Drug Targets
Biophysical & Biochemical Services to Characterize Target Interaction
Established Assays
Optimized assay conditions
Flexible
Single/multiple assays in parallel
Cost-effective
High quality data
Fast Turnaround Time
Less than 2 weeks
nanoDSF – MST – SPR – ADP-Glo – Nucleotide exchange
Protein Supply
Established protein constructs in-house
Tailored high quality assay grade proteins
Protein QC: SDS-PAGE, aSEC, MS
Complete protein supply included
Assay Initiation & Measurements
Established assay conditions
Established labeling/coupling method
Published tool compounds
Up to 3 Tms / Kds / IC50s included
Results & Report
A tabulated report included
Extended report available including measured curves, assay conditions, analysis and scientific summary
Biophysical Assays covering a Broad Range of Drug Targets
| Target | UniProt ID | PP | MST | nanoDSF | SPR | Biochemical Assay |
| CDK7 | P50613 | √ | √ | √ | √ | _ |
| CRBN/DDB1 | Q96SW2/Q16531 | √ | √ | √ | developing | _ |
| cREL | Q96HD1 | √ | √ | √ | _ | _ |
| DOCK5 | Q9H7D0 | √ | √ | √ | √ | nucleotide exchange |
| GLUT1 | P11166 | √ | √ | √ | _ | _ |
| GRB2 | P62993 | √ | √ | √ | _ | _ |
| KRAS | P01116 | √ | √ | √ | √ | nucleotide exchange |
| MALT1 | Q9UDY8 | √ | √ | √ | √ | _ |
| MAP4K1 | Q92918 | √ | √ | √ | developing | ADP Glo |
| NLRP3 | Q96P20 | √ | √ | √ | developing | ADP Glo |
| NRAS | P01111 | √ | √ | √ | √ | nucleotide exchange |
| P2RX3 | P56373 | √ | √ | √ | _ | _ |
| p38 | Q15759 | √ | √ | √ | _ | _ |
| PolQ | O75417 | √ | √ | √ | _ | _ |
| SHP2 | Q06124 | √ | √ | √ | _ | _ |
| SMARCA2 | P51531 | √ | √ | √ | developing | ADP Glo |
| SOS1 | Q07889 | √ | √ | √ | _ | nucleotide exchange |
| STAT3 | P40763 | √ | _ | √ | √ | _ |
| STAT4 | Q14765 | √ | _ | _ | √ | _ |
| STAT6 | P42226 | √ | √ | √ | √ | _ |
| STING | Q86WV6 | √ | √ | √ | √ | _ |
| USP7 | Q93009 | √ | √ | √ | √ | _ |
| WRN | Q14191 | √ | √ | √ | √ | _ |
View Examples from our One Stop Target-to-Hit Series:
Case Study: biophysical assays to identify novel K-RAS inhibitors
K-RAS is a member of the RAS protein family – GTPases which are involved in signaling processes leading to cell growth and proliferation. Oncogenic variants contribute to 25% of cancers including colorectal and lung cancer. This makes the RAS family of proteins important targets for cancer treatment. After 30 years of research, the recently developed K-RAS inhibitor (Canon et al., 2019) opened the door for promising strategies to target this protein family.
To support and accelerate drug development campaigns to identify novel K-RAS inhibitors, WuXi AppTec offers a platform for small molecule hit-finding and lead optimization including biophysical assays and structure biology services based on established systems.
Protein Production
- Broad variety of constructs for biophysical assays and crystallography established including,
- wild type
- G12C, G12D, G12V
- G13D
- “Cys-light” variants for covalent inhibitors
- Nucleotide exchange protocols established to provide K-RAS variants loaded with GDP and alternative nucleotide analogues such as GTPyS or GMPPNG GDP
- Characterization and optimization of covalent complex formation using HPLC-MS
- Related targets protein interaction partners such as SOS1 and Raf available
Biophysical assays for different K-RAS variants established as “Ready-to-Go”
nanoDSF
Nucleotide exchange assay
Labeled MST
GFP-KRAS Fusion
MST in eukaryotic cell lysates
Crystallography
- Established co-crystallization system for covalent and non-covalent small molecule inhibitors
- Non-covalent and covalent inhibitors; GDP and non-hydrolysable GTP analog bound states
- Rapid data collection – K-RAS data sets up to 1.3 Å resolution collected in-house on a Bruker MetalJet
- Established crystallization system for related targets e.g.: SOS1, K-RAS-SOS1 complex
