| Type
of services targeting GPCRs |
Brief
Description |
Assays and
Modes Available |
Formats
Offered |
Standard TAT |
Customization
Possibilities |
| GPCR Binding Assays |
| Radiometric
binding assay |
Competitive radioligand
binding assays |
> 130 assays offered
covering 111 targets |
From stand-alone assays
(1 Dose and DRCs for IC50 and Ki determination) to MTS campaigns or profiling
solutions |
15 Days |
Yes (e.g. allosteric modulation of orthosteric ligand
binding, kon/koff binding kinetics, tailored assay developments from client’s
radioligand or cells, non-human ortholog assays…) |
| GPCR Functional Assays |
| IP1
assays and Ca++ assays |
Largest range of functional assays to investigate IP-1 and
Ca2+ GPCR-related pathways (Gq and Gα15) |
> 200 assays (agonist & antagonist modes) for over
100 targets |
TR-FRET/HTRF, Fluo-4 and Fluo-8 |
15-20 days |
Yes (e.g. custom ligand and assay conditions, PAM studies,
GPCR hit finding cascades…) |
| cAMP
assays |
Screening and profiling of your compounds to investigate
cAMP modulation (Gi and Gs) |
> 110 tests (agonist & antagonist) mode for over 75
targets |
TR-FRET/HTRF assays compatible with HTS campaigns and
profiling programs (1 Dose and/or DRC for EC50 /
IC50 determination) |
15-20 days |
Yes (e.g. Custom ligand and assay conditions, PAM studies,
HTS programs…) |
| Full functional GPCR panel |
The Full Functional GPCR Panel is a comprehensive panel
covering 164 GPCRs with robust cell-based second messenger assays (measuring
Ca2+, IP1 or cAMP) in agonist/antagonist modes |
328 assays (agonist & antagonist assays for 164 GPCRs) |
TR-FRET/HTRF, Fluo-4 and Fluo-8 . Available for 1 Dose
and/or DRC for EC50 / IC50 determination |
30 days |
|
| GTPgammaS
functional assays |
Determination of the
binding of the non-hydrolyzable analog [35S]GTPγS to Gα subunits. GTPγS
assays evaluate an early event after GPCR activation and are able to
discriminate full or partial agonists, neutral antagonists, inverse agonists,
allosteric regulators |
> 95 assays covering
over 30 targets (agonist, inverse agonist & antagonist modes) |
Detection by
scintillation for stand-alone to MTS and profiling methods. Dose response
format at 8 concentrations in duplicate |
20 days |
Yes, custom ligand,
custom assay condition, compound combination and PAM study |
| GPCR Functional Assays using EFC β-arrestin cells |
| β-arrestin
recruitment assays |
Assays utilize β-arrestin recruitment to rapidly,
reproducibly and reliably profile compounds in a G-protein independent
pathway. |
> 336 Assays offered in Agonist, Antagonist, PAM and NAM
mode. Some assays offered in Inverse Agonist mode |
Primary screening at one or more concentrations.
Dose response format at 10 concentrations in duplicate. Assays are also
available for HTS screens |
15 days |
Yes, custom ligand, custom buffer and EC50 shift |
| cAMP assays |
HitHunter® cAMP assays are competitive immunoassays that
utilize EFC. Beta arrestin assays can also be used to monitor cAMP levels by
TR-FRET. |
> 390 Assays are offered in Agonist, Antagonist, PAM and
NAM modes |
Primary
screening at one or more concentrations.
Dose response format at 10 concentrations in duplicate. Assays are also
available for HTS screens |
15 days |
Yes, custom ligand, custom buffer, EC50 shift, choice
of using HitHunter or TR-FRET format |
| GPCR
Internalization |
GPCR Internalization Assays are functional cell-based assays
that measure GPCR endocytosis using β-arrestin cells |
> 298 Assays measure total internalization or activated
internalization |
Primary screening at one or more concentrations. Dose
response format at 10 concentrations in duplicate |
15 days |
Yes, custom ligand or custom buffer |
| gpcrMAX panels |
Largest panel of gpcr assays offered in β-arrestin format |
336 Assays |
Panel offered to measure agonist and antagonist activity at
one concentration duplicate. |
22 days |
|
| orphanMAX panel |
Largest panel of orphan gpcr assays offered in β-arrestin
format |
73 Assays |
Panel offered to measure agonist activity at one
concentration duplicate. |
22 days |
|
| obesityLITE
Panel |
Panel of GPCR β-arrestin or second messenger assays and
cytokine assay that can be used to measure specificity or selectivity during
Hit to Lead or Lead Optimization stages of drug development. |
25 Assays (agonist or antagonist mode) |
Panel offered to measure agonist or antagonist activity in
Dose response format at 10 concentrations in duplicate |
22 days |
|
| gpcrBIAS |
Compound profiling using
second messenger, β-arrestin or internalization assays from a choice of >
150 GPCRs. Any two assay systems are chosen to measure bias |
> 150 Assays |
Dose response curves are
performed in quadruplicate to measure GPCR responses for any two assay
systems. Assay choices include 2nd messenger signaling, β-Arrestin
recruitment, and receptor internalization. Experiments with the natural
ligand and test substance are performed in parallel. |
15 days |
|
| Chemokine
Panel |
Panel of Human Chemokine GPCR cell based assays that can be
used to measure specificity or selectivity during Hit to Lead or Lead
Optimization stages of drug development. |
38 Assays (agonist or antagonist mode) |
Panel offered to measure agonist or antagonist activity at 1
concentration in duplicate |
22 days |
|