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GPCR Screening & Profiling Trends 2013 by HTStec Ltd. is now available at
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This
market report summarizes the results of HTStec's 5th industry-wide global
web-based benchmarking survey on GPCR screening and profiling carried out in
August 2013. The survey was initiated by HTStec as part of its tracking of life
science marketplaces. The questionnaire was compiled to meet the needs,
requirements and interests of the GPCR vendor community. The objectives were to
comprehensively document current practices and preferences in GPCR primary
screening and compound profiling, and to understand future user requirements,
particularly with respect to the need for new assays, approaches and the use of
outsourced services. The aim was to compile a reference document on GPCR
screening and profiling metrics, which could be directly compared with HTStec's
previous reports (the last one on GPCRs was published in October 2010). Equal
emphasis was given to soliciting opinion from Pharma, Biotech and Academic
Research market segments in both North America and Europe.
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The survey
looked at both in house and outsourced GPCR primary screening and compound
profiling, as practiced today (2013) and in some cases as predicted for the
future (2015). Specifically the following were investigated: whether the number
of GPCR primary screening targets or programs under investigation is changing;
the proportion of GPCR screens that are cell-based and orphan receptors; use of
different methods for assaying GPCR activation; preferred assay readout
technology and supplier for GPCR screening; proportion of GPCR Ca2+ flux assays
that are fluorescence-based; number of GPCR primary screens and wells per
screen; approach to GPCR profiling; preferred assay readout technology and
supplier for GPCR profiling; size of in house profiling panels and total wells
profiled in house per year; how receptor panels are chosen; level of interest
in outsourcing; methods of assaying GPCR activation that respondents wish to
access by outsourcing; type of GPCR panels most interested to access at a
fee-for-service provider; typical sizes of outsourced GPCR profiling panels
used and total wells profiled per year at a fee-for-service providers; most
trusted and most used providers of outsourced GPCR assay services; in house and
outsourced budgets for GPCR screening and profiling; the breakdown of in house
budgets; average costs paid per well for GPCR screening and profiling; level of
interest in new assays/approaches for GPCR screening and profiling; suitability
of available tools for new assays/approaches for GPCR screening and profiling;
the proportion of GPCR assays that are made using primary cell lines and stem
cell derived phenotypes; main barriers to the implementation of a new GPCR
screening technology; where a GPCR reagent developer or assay fee-for-service
provider should focus their efforts in the future; preferred way of sourcing
GPCR expressing cell lines and the factors that drive decision making when
sourcing; and any unmet needs in GPCR screening & profiling today.
The main
questionnaire consisted of 30 multi-choice questions and 1 open-ended question.
In addition, there were 7 questions related solely to survey demographics. The
survey collected 96 validated responses, of these 66% provided comprehensive
input. Survey responses were geographically split: 61% North America; 27%
Europe; 7% Asia (excluding Japan); and 5% Japan. Survey respondents were drawn
from persons or groups involved in GPCR primary screening and compound
profiling in house and the outsourcing of GPCR testing to fee-for-service
providers. Respondents came from 21 Large Pharma; 21 University; 17 Biotech; 12
Medium-Small Pharma; 9 Hospital/Clinic/Medical School; 6 Research Institute; 5
Academic Screening Center; 4 Government Laboratory; and 1 Other.
Most
survey respondents had a senior job role or position which was in descending
order: 17 senior scientists/researchers; 17 principal investigators; 13
research scientists; 13 professors/assistant professors; 8 directors; 7
section/group leaders; 7 department heads; 1 graduate/PhD student; 1 vice
president; and 1 outsourcing manager.
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Respondents
main group activities were: 27 basic research; 23 a combination of drug
discovery roles; 11 assay development; 10 primary screening (HTS); 8 applied
research; 7 hits-to-leads (lead optimization); 6 therapeutic areas; 2 secondary
screening; and 2 compound profiling. Survey results were expressed as an
average of all survey respondents. In addition, where appropriate the data was
fully reanalyzed after sub-division into the following 5 survey groups: 1)
Pharma; 2) Biotech; 3) Academic Research; 4) Europe; and 5) North America.
The median
number of GPCR primary screening targets/programs under investigation in 2013
was 3. 70% of GPCR primary screens were cell-based and 17% were orphan
receptors in 2013. In 2013 the relative use of different methods used to study
GPCR activation was: 24% binding assays; 16% cAMP or cGMP assays; 13% Ca2+
flux/mobilization assays; 12% β-arrestin recruitment or receptor
internalization; and 11% reporter gene assays. All other methods had less than
10% use. The preferred GPCR readout technologies and suppliers for GPCR
activation assays used in both primary screening and compound profiling were as
follows: binding assays - radiometric from PerkinElmer; β-arrestin recruitment
or receptor internalization - chemiluminescence from DiscoveRx; label-free
cellular changes & translocation - label-free readout from Corning; GTP
γS -
radiometric from PerkinElmer; reporter gene assays - glow luminescence from
Promega ; Ca2+ flux/mobilization assays - fluorescence intensity from Molecular
Devices; IP3 or IP1 - TR-FRET from Cisbio; cAMP or cGMP Assays - TR-FRET from
Cisbio; ERK phosphorylation assays - TR-FRET from PerkinElmer; and other
phenotypic readouts - various readouts and suppliers. 44% of all GPCR Ca2+
flux/mobilization assays were fluorescence-based in 2013.
Median in
house 2013 GPCR screening metrics were: 3 primary screens/year and 10K-25K
wells/screen. The preferred approach to GPCR profiling was to profile selected
lead compounds only in house. Median in house 2013 GPCR profiling metrics were:
2 to 3 new receptors added to the panel per year; a total of 6 to 10 receptors
per panel; and 5K-10K wells profiled per year. Respondents did not have a
preferred way of choosing panels when running GPCR compound profiles.
42% of
respondents might outsource GPCR primary screening versus 57% might outsource
GPCR compound profiling today (2013). Most want to access primary screening
using β-arrestin recruitment or receptor internalization methods and compound
profiling using binding assays methods. The types of GPCR panels respondents
were most interested in accessing for outsourced compound profiling today
(2013) were those that included all known GPCRs available. The median
outsourced 2013 GPCR profiling metrics were: 6 to 10 receptors/profile and
1K-15K wells profiled per year.
PerkinElmer,
Life Technologies and Cerep were ranked the most trusted and most used
outsourced GPCR fee-for-service providers. Although no provider stood out way
above all others. The median GPCR primary screening budget allocations in 2013
were $10K-$25K/lab in house and $5K-$10K/lab outsourced. The biggest
expenditure was on bulk reagents & pre-packaged assay kits.
The median
GPCR compound profiling budget allocations in 2013 were $10K-$25K/lab in house
and lt;$5K/lab outsourced. The biggest expenditure was on bulk reagents &
pre-packaged assay kits. The median cost/well for GPCR primary screening in
2013 was $0.35-$0.50/well both in house & outsourced.
The median
cost per well for GPCR compound profiling in 2013 was $0.35-$0.5/well in house
versus $0.50-$0.75/well outsourced. Functional selectivity was rated the
assay/approach for GPCR primary screening and compound profiling that
respondents had most interest in using/evaluating. Receptor internalization and
trafficking was the assay/approach for GPCR primary screening and compound
profiling where the suitability of currently available tools was rated most
effective.
24% of
GPCR assays were made using primary cells and 6% using stem cell derived
phenotypes in 2013. Instrumentation/technology costs were the most significant
barrier to new GPCR technology adoption. Receptor internalization and
trafficking was rated as the area where respondents thought GPCR reagent
developers should focus their efforts going forward. Offer screening services
in more biologically relevant cellular backgrounds was rated as the area where
respondents thought GPCR fee-for service providers should focus their efforts
going forward.
Most
respondents prefer to source GPCR expressing cell lines by making them in
house. Cost and time were ranked the most important factors when
making/sourcing GPCR expressing cell lines. Feedback on some unmet needs that
exist today in GPCR screening and profiling were documented. Several bottom-up
models were developed around the respondent's annual budgets to estimate the
global markets for GPCR screening and profiling. In 2013 these markets were
estimated to be as follows: in house GPCR primary screening reagents - $144M;
in house GPCR compound profiling reagents - $28M; outsourced GPCR primary
screening - $20M; and outsourced GPCR compound profiling - $24M. The market was
segmented by organization and geography. CAGR estimates for 2015 were made for
the market segments.
The full
report provides the data, details of the breakdown of the responses for each
question, its segmentation and the estimates for the future (2015). It also
highlights some interesting differences, particularly between Pharma versus the
other survey groups.
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