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Results for "

PK-PD

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Casein Kinase (1) COX (1) EGFR (1) ERK (1) FAK (1) Fluorescent Dye (1) GPR84 (1) JNK (1) LPL Receptor (1) p38 MAPK (1) Phosphodiesterase (PDE) (1) PI3K (1) PROTACs (1) TNF Receptor (1) γ-secretase (2)
By Research Areas:	Cancer (4) Inflammation/Immunology (3) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: PD-1/PD-L1 DNA-PK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-132296

GSK215 1 Publications Verification	FAK PROTACs	Cancer
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC₅₀ of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .

HY-151813

NNMT-IN-4	Fluorescent Dye	Cancer
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC₅₀ values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .

HY-135303

GLPG1205 5+ Cited Publications	GPR84	Inflammation/Immunology
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-117482

BPN-15606	γ-secretase	Neurological Disease
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .

HY-123637

Autotaxin-IN-1	Phosphodiesterase (PDE)	Inflammation/Immunology
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC₅₀=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain .

HY-15495B

(3S)-Tanzisertib hydrochloride (3S)-CC-930 hydrochloride	JNK ERK p38 MAPK EGFR TNF Receptor	Inflammation/Immunology
(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC₅₀ values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC₅₀ = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research .

HY-19500

SC-75416	COX	Others
SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.

HY-117482A

BPN-15606 besylate	γ-secretase	Neurological Disease
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .

HY-16622A

GSK 1842799 TFA	LPL Receptor	Others
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .

HY-146260

NVP-CLR457	PI3K	Cancer
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .

HY-178980

APL-5125	Casein Kinase	Cancer
APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC₅₀ of 0.348 nM and a K_i of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .

Cat. No.	Product Name

HY-L904

Drug Fragment Library	1,332 compounds
The MCE 1K Drug Fragment Library consists of 1,168 drug fragments. These drug fragments are derived from 2,946 FDA-approved drug molecules, and fragments from one drug can appear in other drugs, so these fragments are somewhat correlated with good PK/PD properties. Fragment-based screening can reserve enough chemical space for subsequent structural optimization. This compound library is an essential tool for drug screening based on FBDD (Fragment-Based Drug Discovery).

Drug Fragment Library

1,332 compounds

The MCE 1K Drug Fragment Library consists of 1,168 drug fragments. These drug fragments are derived from 2,946 FDA-approved drug molecules, and fragments from one drug can appear in other drugs, so these fragments are somewhat correlated with good PK/PD properties. Fragment-based screening can reserve enough chemical space for subsequent structural optimization. This compound library is an essential tool for drug screening based on FBDD (Fragment-Based Drug Discovery).

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