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High-throughput kinetic system for small-molecule drug discovery

Award Number: R44TR005335
ORGANIZATION: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/15/2026
PERIOD OF PERFORMANCE END DATE: 08/31/2028

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High-throughput kinetic system for small-molecule drug discovery - Abstract Evidence is accumulating for higher efficacy of small molecule drugs that have off-rates slower than the pharmacokinetic clearance rate. Despite the importance of kinetics, the standard approach is low throughput Biacore testing in de novo drug discovery/screening. But we offer a new way that outruns commercial plate readers. Capienda Biotech is developing the first instrument offering rapid kinetics for competitive inhibitors at high throughput for drug discovery and optimization. Advancing upon our NSF SBIR Phase I success in building a prototype instrument for highly parallel assays and sensitive detection for binding kinase targets (128 tests simultaneously), we propose the Phase II commercial instrument (up to 384 tests simultaneously) with hardware upgrade for higher-throughput kinetics. The innovative instrument design and assay chemistry enables us to characterize compounds that target human kinases for inflammatory indications and oncology. The approach is expected to be applicable across a growing portfolio of >500 kinases. Selectivity of kinase inhibitors is a major issue in targeting this class of drug targets. Drugs for auto-immune and anti-inflammatory indications have been approved by the FDA. Sixteen small molecule inhibitors target kinases regulating the immune system. Ruxolitinib, baricitinib, momelotinib, tofacitinib and fostamatinib specifically bind the intended kinases in immune signaling (JAKs or SYK) and have little unintended binding to typical kinases targeted by oncology drugs, all without hematologic abnormalities (neutropenia, thrombocytopenia or anemia). By contrast, cancer drugs ponatinib, dasatinib and danusertib bind their intended targets (BRC-ABL and aurora kinases) and also multiple off-target kinases that regulate the immune system including BTK, LYN, LCK, FYN and MAPK p38α, but in the clinic patients often experience neutropenia, thrombocytopenia and anemia. Just as Pharma focuses drug discovery against one target, we propose to develop a high throughput application targeting BRAF to characterize binding kinetics of small molecule compounds. Further, we propose to develop assays for kinase selectivity to characterize kinetics of compounds binding to off-target kinases ABL1, LYN, LCK and FYN. We will measure kinetic parameters: kon, koff, drug residence time, dissociation half-life and determine Kd. The proposed targeted application and selectivity application will enable Medicinal Chemists to distinguish between promising vs. unpromising compounds for long duration of action and improved pharmacokinetics. In the longer run, kinome-wide examination of compounds early on and throughout the drug discovery process may minimize polypharmacology and adverse events in the clinic. This proposal addresses an unmet analytical need in drug discovery, which will open a bottleneck in the path to new, highly specific medicines. We will establish a process for optimization, validation, workflow and data processing. We will demonstrate a systematic approach to kinetic targeting of kinases by a chemistry + instrument system. The solution offers a systematic high-throughput approach that will lead to better drugs entering clinical trials.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2027 ( Subtotal = $0 )
2027	2026	CAPIENDA BIOTECH, LLC	13225 SUNDANCE AVE	SAN DIEGO	CA	92129	SAN DIEGO	USA	National Center for Advancing Translational Sciences	000	2	10/14/2026	COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2026 ( Subtotal = $1,401,698 )
2026	2026	CAPIENDA BIOTECH, LLC	13225 SUNDANCE AVE	SAN DIEGO	CA	92129	SAN DIEGO	USA	National Center for Advancing Translational Sciences	000	2	9/17/2026	COMPETING CONTINUATION	$1,401,698
														Subtotal = $1,401,698

Grand Total All Awards = $1,401,698

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High-throughput kinetic system for small-molecule drug discovery

Award Number: R44TR005335

ORGANIZATION: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/15/2026

PERIOD OF PERFORMANCE END DATE: 08/31/2028

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