Tomorrow, 11 AM ET / 8 AM PT. Functional Volume Control, live with Dr. Terry Kenakin. With @EurofinsDscvrx. Registration open until we go live. https://t.co/cLaNTK3F45
#DrGPCR#GPCR
Two days out. A positive allosteric modulator can turn out to be a direct agonist once the system is sensitive enough. A PAM and a PAM-agonist are not the same molecule. Assay volume control, live Sept 24. With Eurofins DiscoverX. https://t.co/cLaNTK3F45
#DrGPCR#GPCR
Next Thursday, September 24. A high affinity, low efficacy agonist can run out of gas in an insensitive tissue and produce no response. Volume control uncovers that. In collaboration with Eurofins DiscoverX. https://t.co/cLaNTK3F45
#DrGPCR#GPCR
A compound can look silent and still carry low efficacy. Raise the system's sensitivity and it appears, and it could produce agonism in a sensitive tissue. Assay volume control, live Sept 24. In collaboration with Eurofins DiscoverX. https://t.co/cLaNTK3F45
#DrGPCR#GPCR
On September 24 at 11 AM ET / 8 AM PT, a live session on assay volume control. Reduce a system's sensitivity to measure affinity and efficacy, increase it to reveal what was hidden. https://t.co/cLaNTK4cTD
#DrGPCR#GPCR
Two opposing activities can cancel at steady state and leave a flat number.
First-anniversary gift for Kenakin Brief subscribers through Sep 2026. Subscribe free, code goes out in the Tuesday email: https://t.co/rj5oTehY0u
#DrGPCR#GPCR
First-anniversary gift for Kenakin Brief subscribers through Sep 2026. Subscribe free, code goes out in the Tuesday email: https://t.co/rj5oTehY0u
#DrGPCR#GPCR
A regression can fit perfectly and still be wrong. Schild analysis assumes competition at the orthosteric site; when that quietly fails, the plot stays clean and the conclusion does not
Terry's Corner turns one. A year of pharmacological thinking with Dr. Kenakin, 32 lessons deep.
To mark it, the door is open at the founding price for Kenakin Brief subscribers through Sep. Subscribe free, code goes out in the Tuesday email: https://t.co/rj5oTehY0u
#DrGPCR#GPCR
This Thursday's AMA with Dr. Kenakin has a time change: 1 pm EST, June 25. Topic: assay volume control as a tool for GPCR research. Free for Kenakin Brief subscribers. https://t.co/rj5oTehY0u #GPCR#DrugDiscovery#DrGPCR
Why is orthosteric small-molecule agonism at family B GPCRs a harder problem than at smaller receptors? The structural account locates the difficulty in geometry, not chemistry. New TC session from @TerryCornerHQ . #DrGPCR#GPCR https://t.co/7gjdWOQd2N
Live with Dr. Terry Kenakin, May 28 at 11 AM EST.
Signaling Bias as a Drug Candidate Property. The biology, the assays, and how the data inform lead selection.
With @EurofinsDscvrx. Free.
https://t.co/iNRHWjXvnv #DrGPCR#GPCR
May 14. @Pharmechanic on GPCR signaling kinetics and drug action. Temporal dynamics drive therapeutic outcomes beyond binding affinity predictions. Live session, direct expert access. https://t.co/oKdLoJWZRT #DrGPCR#GPCR#SignalingKinetics
Classical beta-2 agonists all hit the same wall: desensitization. @StockholmUni professor Tore Bengtsson built one that doesn't, and it's heading into Phase 2. 🎧 New episode out now. https://t.co/LwJIHFIodN
#DrGPCR#GPCR
GPCR signaling kinetics shape therapeutic outcomes beyond what binding affinity predicts. @Pharmechanic on measuring temporal dynamics and translating kinetic insights into drug discovery. Dr. GPCR Masterclass, May 14. https://t.co/oKdLoJWs2l #DrGPCR#GPCR#GPCRKinetics
Live webinar, May 28 at 11 AM EST.
Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates, with Dr. Terry Kenakin (@UNC | @TerryCornerHQ )
In collaboration with @EurofinsDscvrx. Free. Recording after.
https://t.co/sAAulff36j
#DrGPCR#GPCR
Five GPCR Masterclasses before summer — kinetics, spatial biology, subcellular regulation, program building, orphan receptors. Two April recordings into the library next week. Community in Boston next week. https://t.co/c3tgJlAFp9
#gpcr#drgpcr
Spring break for Terry's Corner this week. Back next week: biologics for GPCRs — where small molecule rules quietly stop applying and the therapeutic landscape opens up differently.
#DrGPCR#GPCR
https://t.co/rj5oTehY0u
Orthosteric binding hijacks the target. Allosteric binding works with it. Two modes — fundamentally different pharmacological consequences.
This month's AMA with Dr. Terry Kenakin: how to differentiate them, and why it matters before you go further.
#DrGPCR#GPCR