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Structure-based drug discovery for Dopamine D2 Receptor Selective Ligands

Award Number: R44MH115875
ORGANIZATION: NATIONAL INSTITUTE OF MENTAL HEALTH
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 07/01/2017
PERIOD OF PERFORMANCE END DATE: 03/31/2024

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Structure-based drug discovery for Dopamine D2 Receptor Selective Ligands - Summary The neurotransmitter dopamine (DA) controls many central nervous system functions through three major pathways in the brain, the tuberoinfundibular, the nigrostriatal and the mesocorticolimic (mesocortical and mesolimbic). Each is associated with different processes, and dysfunction can lead to varying diseases and disorders of the central nervous system (CNS). There are five known DA receptors, D2 (D2R) is one of the most abundant DA receptors in the brain, and is thus an important pharmacological target for many CNS diseases. Most of the clinically efficacious antipsychotics used for the treatment of schizophrenia and Parkinson's disease, which are associated with the mesocorticolimbic and nigrostriatal pathways, are D2R agonists or antagonists. However, new drugs with improved efficacy and side-effect profiles are needed for these relatively prevalent diseases. In addition, several drugs abused by humans affect DA neurotransmission in the mesolimbic pathway, due to their effects on reward-related behaviors. Therefore D2R is also a focus for the discovery of pharmacological treatments for substance abuse of a certain class of drugs and addiction disorders for which there are none currently available. The goal of this proposal is to discover novel D2R selective small molecule ligands that can be developed for the treatment of disorders of the CNS. Utilizing a combination of D2R three-dimensional structures, including the active-state structure obtained during our Phase I studies, virtual screening and DNA- encoded library screening, we will identify and develop novel lead compounds. These D2R targeted compounds will be optimized and undergo pre-clinical studies at which point we will seek commercial collaboration with a large pharmaceutical company. This proposal is in response to the Funding Opportunity Announcement PA-18- 574, “PHS 2018-02 Omnibus Solicitation of the NIH, CDC, and FDA for Small Business Innovation Research Grant Applications (Parent SBIR [R43/R44] Clinical Trial Not Allowed)”.


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: 2024 ( Subtotal = $0 )
2024	2021	CONFOMRTRX INC	840 CHIMALUS DR	PALO ALTO	CA	94306	SANTA CLARA	USA	Mental Health Research Grants	000	4	8/1/2024	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2023 ( Subtotal = $0 )
2023	2021	CONFOMETRX	840 CHIMALUS DR	PALO ALTO	CA	94306	SANTA CLARA	USA	Mental Health Research Grants	000	4	7/15/2023	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2021 ( Subtotal = $738,119 )
2021	2021	CONFOMETRX	840 CHIMALUS DR	PALO ALTO	CA	94306	SANTA CLARA	USA	Mental Health Research Grants	000	4	6/24/2021	NON-COMPETING CONTINUATION	$738,119
														Subtotal = $738,119

Issue Date FY: 2020 ( Subtotal = $764,531 )
2020	2020	CONFOMETRX	840 CHIMALUS DR	PALO ALTO	CA	94306	SANTA CLARA	USA	Mental Health Research Grants	000	3	7/7/2020	NON-COMPETING CONTINUATION	$764,531
														Subtotal = $764,531

Issue Date FY: 2019 ( Subtotal = $659,183 )
2019	2019	CONFOMETRX	840 CHIMALUS DR	PALO ALTO	CA	94306	SANTA CLARA	USA	Mental Health Research Grants	000	2	7/18/2019	COMPETING CONTINUATION	$659,183
														Subtotal = $659,183

Grand Total All Awards = $2,161,833

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Structure-based drug discovery for Dopamine D2 Receptor Selective Ligands

Award Number: R44MH115875

ORGANIZATION: NATIONAL INSTITUTE OF MENTAL HEALTH

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 07/01/2017

PERIOD OF PERFORMANCE END DATE: 03/31/2024

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