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Kinetics for Drug Discovery (K4DD)

Objective

There is mounting evidence that the often ignored kinetic aspects of the interaction between a drug and its target are highly relevant for clinical success. This ignorance may be one of the reasons for the high attrition rates in drug discovery, as it has been analyzed that many recently marketed drugs had indeed improved kinetic profiles.
This hindsight knowledge needs to be converted into data-driven guidelines and easily accessible high-throughput assays for future drug discovery and fuels the K4DD consortium of over 20 partners, EFPIA members, universities, research institutes and SMEs. Our integrated approach will lead to the definition of any compound in terms of its target ‘kinotype’, next to affinity and selectivity. For us, integration means analyzing the kinetic behavior of different targets (GPCRs, kinases, proteases) across the three work packages. The partners in the consortium are European key players: they elucidate(d) structures of GPCRs and kinases, are at the forefront of bioanalytical techniques, e.g. surface plasmon resonance, are world-leaders in PKPD modeling, and bring the best of computational resources for e.g. molecular dynamics calculations. Thus, we study the drug-target interaction from picoseconds to >hours, for both soluble and membrane-bound proteins.
At the end of the consortium’s lifetime we anticipate that kinetic aspects of the drug-target interaction can routinely be studied in robust and accessible assays within and outside the consortium, that editors and reviewers routinely ask for a compound’s kinetic data next to its affinity and selectivity, that ‘kinotypic’ knowledge helps define the target product profile and guide the subsequent lead finding and optimization process, and that kinetic guidelines for predictive PKPD modeling approaches are the logical consequence of our efforts.
Thus, the overall ambition of the consortium is to instill lasting kinetic awareness into the pharma community.

Call for proposal

IMI-JU-04-2011
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Coordinator

BAYER AKTIENGESELLSCHAFT
Address
Kaiser-wilhelm-allee 1
51373 Leverkusen
Germany

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Principal investigator
Anke Mueller-Fahrnow (Dr.)
Administrative Contact
Burkhardt Neumann (Mr.)

Participants (20)

UNIVERSITEIT LEIDEN
Netherlands
EU contribution
€ 1 687 262
Address
Rapenburg 70
2311 EZ Leiden

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Ton Brouwer (Mr.)
STICHTING VU
Netherlands
EU contribution
€ 819 999
Address
De Boelelaan 1105
1081 HV Amsterdam

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Dirkje Schinkelshoek (Drs.)
UNIVERSITY OF DUNDEE
United Kingdom
EU contribution
€ 1 000 899
Address
Nethergate
DD1 4HN Dundee

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Zoe Kidd (Mrs)
HITS GGMBH
Germany
EU contribution
€ 506 000
Address
Schloss Wolfsbrunnenweg 35
69118 Heidelberg

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Activity type
Research Organisations
Administrative Contact
Baerbel Mack (Mrs.)
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD
United Kingdom
EU contribution
€ 667 549
Address
Wellington Square University Offices
OX1 2JD Oxford

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Linda Pialek (Ms)
IMPERIAL COLLEGE OF SCIENCE TECHNOLOGY AND MEDICINE
United Kingdom
EU contribution
€ 534 757
Address
South Kensington Campus Exhibition Road
SW7 2AZ London

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Brooke Alasya (Miss)
Heptares Therapeutics Limited
United Kingdom
EU contribution
€ 444 000
Address
Broadwater Road
AL7 3AX Welwyn Garden City

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Administrative Contact
Simon Rodgers (Dr)
THE UNIVERSITY OF NOTTINGHAM
United Kingdom
EU contribution
€ 407 999
Address
University Park
NG7 2RD Nottingham

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Paul Cartledge (Mr)
RUHR-UNIVERSITAET BOCHUM
Germany
EU contribution
€ 404 999
Address
Universitaetsstrasse 150
44801 Bochum

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Jörn Güldenhaupt (Dr.)
European ScreeningPort GmbH

Participation ended

Germany
EU contribution
€ 141 492
Address
Schnackenburgallee
22525 Hamburg

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Mira Grättinger (Dr.)
Sierra Sensors GmbH
Germany
EU contribution
€ 222 771
Address
Falkenried
20251 Hamburg

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Klaus Wiehler (Dr.)
ASTRAZENECA AB
Sweden
Address
Vastra Maelarhamnen
151 85 Sodertaelje

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Eva Lindgren (Senior Director)
GLAXOSMITHKLINE RESEARCH AND DEVELOPMENT LTD.
United Kingdom
Address
Great West Road 980
TW89GS Brentford

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Sally Miles (-)
JANSSEN PHARMACEUTICA NV
Belgium
Address
Turnhoutseweg 30
2340 Beerse

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Henk Sipma (Dr)
MERCK KOMMANDITGESELLSCHAFT AUF AKTIEN
Germany
Address
Frankfurter Strasse 250
64293 Darmstadt

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Ninog Péresse (Ms)
F. HOFFMANN-LA ROCHE AG
Switzerland
Address
Grenzacherstrasse 124
4070 Basel

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Jason Hannon (Mr.)
SANOFI-AVENTIS DEUTSCHLAND GMBH
Germany
Address
Bruningstrasse 50
65929 Frankfurt Am Main

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Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Matthias Dreyer (Dr.)
STICHTING LYGATURE
Netherlands
EU contribution
€ 639 643
Address
Jaarbeursplein 6
3521 AL Utrecht

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Activity type
Other
Administrative Contact
Denis Groot (Mr.)
UNIVERSITAT WIEN
Austria
EU contribution
€ 404 060
Address
Universitatsring 1
1010 Wien

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Activity type
Higher or Secondary Education Establishments
Administrative Contact
Helmut Schaschl (Dr.)
FRAUNHOFER GESELLSCHAFT ZUR FORDERUNG DER ANGEWANDTEN FORSCHUNG EV
Germany
EU contribution
€ 405 500
Address
Hansastrasse 27c
80686 Munchen

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Activity type
Research Organisations
Administrative Contact
Michael Prestele (Mr.)