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538

阻害剤

天然化合物

カタログ番号	製品名	別名	ターゲット
T39695	ARD-2128		Androgen Receptor
	ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) degrader of the androgen receptor (AR), effectively diminishing AR protein levels, suppressing AR-regulated gene expression in tumor...		Androgen Receptor
T9497	Niraparib tosylate monohyrate		PARP
	Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting...		PARP
T12266	Ilginatinib	NS-018	Tyrosine Kinases , JAK
	Ilginatinib (NS-018) is a highly active and orally bioavailable inhibitor of JAK2.		Tyrosine Kinases , JAK
T5414	Glumetinib	SCC244	c-Met/HGFR
	Glumetinib (SCC244) (SCC 244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).		c-Met/HGFR
T12266L	Ilginatinib maleate	NS-018 maleate	Tyrosine Kinases , JAK
	Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable inhibitor of JAK2.		Tyrosine Kinases , JAK
T12266L2	Ilginatinib hydrochloride	NS-018 hydrochloride	Tyrosine Kinases , JAK
	Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable inhibitor of JAK2.		Tyrosine Kinases , JAK
T4488	GSK-25	GSK25	ROCK , S6 Kinase , mTOR
	GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).		ROCK , S6 Kinase , mTOR
T3231	Niraparib	MK-4827	Apoptosis , Others , PARP
	Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.		Apoptosis , Others , PARP
T6714	URB-597	KDS-4103,FAAH Inhibitor II	Mitophagy , FAAH , Autophagy
	URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.		Mitophagy , FAAH , Autophagy
T6041	Oprozomib	PR-047,ONX 0912	Proteasome , Autophagy
	Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.		Proteasome , Autophagy
T2119	Venetoclax	GDC-0199,ABT 199,ABT-199,ABT199	BCL , Autophagy
	Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces a...		BCL , Autophagy
T17225	Vercirnon	CCX282-B,GSK-1605786,Traficet-EN	CCR
	Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.		CCR
T9146	Ms48107	Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-	Others
	MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion ch...		Others
T3353	Niraparib hydrochloride	MK-4827 hydrochloride,MK-4827 (hydrochloride)	Apoptosis , Others , PARP
	Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. Niraparib hydrochloride inhibits PARP activity, enhancing the accumulation of...		Apoptosis , Others , PARP
T6892	Niraparib tosylate	MK-4827 (tosylate),MK 4827 tosylate,Niraparib (MK-4827) tosylate	Apoptosis , PARP
	Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor.		Apoptosis , PARP
T15198	Edasalonexent	CAT-1004	NF-κB
	Edasalonexent is an orally bioavailable inhibitor of NF-κB.		NF-κB
T17218	Varespladib methyl	A-002,LY333013	Others , Phospholipase
	Varespladib methyl (LY333013), a bioavailable prodrug of Varespladib, is a selective group II secretory phospholipase A2 inhibitor.		Others , Phospholipase
T10300	AMG2850		TRP/TRPV Channel
	AMG2850 is a potent, orally bioavailable, and selective antagonist of transient receptor potential melastatin 8 (TRPM8).		TRP/TRPV Channel
T11226	ERK1/2 inhibitor 1		ERK
	ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.		ERK
T12847	SB-616234-A	SB-616234A	5-HT Receptor
	SB-616234A is a selective and orally bioavailable antagonist of 5-HT1B receptor, with anxiolytic and antidepressant activity.		5-HT Receptor
T2351	Fasiglifam	TAK875	GPR
	Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.		GPR
T5417	INCB-057643		Apoptosis , Epigenetic Reader Domain
	INCB057643 is a potent, selective and orally bioavailable BET inhibitor.		Apoptosis , Epigenetic Reader Domain
T3389	Antitumor agent-21	TRX818	Others
	Antitumor agent-21 (TRX818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities.		Others
TQ0029	ASTX660		IAP
	ASTX660 is an orally bioavailable dual antagonist of cIAP and XIAP.		IAP
T16776	RO9021		Syk
			Syk
TQ0069	MI-503		Epigenetic Reader Domain , Histone Methyltransferase
	MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.		Epigenetic Reader Domain , Histone Methyltransferase
T17179	Tulrampator	CX-1632,S-47445	iGluR
	Tulrampator (S-47445) is an orally bioavailable positive AMPAR with antidepressant effects.		iGluR
T6123	Verdinexor	KPT-335	CRM1
	Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.		CRM1
T20454	4-Chlorophenylurea	NSC12971,NSC 12971,NSC-12971	Factor Xa
	4-Chlorophenylurea (NSC-12971) is a novel orally bioavailable inhibitor of factor Xa.		Factor Xa
T3544	SHP099 hydrochloride		Phosphatase , Others
	SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor.		Phosphatase , Others
T14901	CCT-251921		CDK
			CDK
T2360	Baricitinib phosphate	Baricitinib Phosphate,LY3009104,INCB-028050 phosphate,LY-3009104 phosphate,INCB028050	Tyrosine Kinases , JAK
	Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1/JAK2 inhibitor.		Tyrosine Kinases , JAK
T39573	GSK251		PI3K
	GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.		PI3K
T6692	TAK-733	TAK733,TAK 733	MEK
	TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.		MEK
T4490	PF-01247324		Sodium Channel
	PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker (IC50: 196 nM).		Sodium Channel
T2259	Silmitasertib	CX-4945	Casein Kinase , Autophagy
	Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).		Casein Kinase , Autophagy
T12395	PDE9-IN-1		PDE
	PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).		PDE
TQ0229	ETP-46321		PI3K
	ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).		PI3K
T6965	RG7112	RG-7112,RG 7112,RO5045337	Mdm2 , E1/E2/E3 Enzyme
	RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.		Mdm2 , E1/E2/E3 Enzyme
T6101	Entospletinib	GS-9973	Syk
	Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.		Syk
T10929L	D-3263 hydrochloride	EC D-3263 HCl,D3263 HCl salt	TRP/TRPV Channel
	D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.		TRP/TRPV Channel
T7667	R1487		p38 MAPK
	R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.		p38 MAPK
T6053	Turofexorate Isopropyl	XL335,FXR-450,WAY-362450	FXR , Autophagy
	Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM		FXR , Autophagy
T12431	PF-06882961		Glucagon Receptor
	PF-06882961 is an orally bioavailable glucagon-like peptide-1 receptor (GLP-1R) agonist.		Glucagon Receptor
T6117	Tivantinib	ARQ 197	Apoptosis , c-Met/HGFR
	Tivantinib (ARQ 197) is an orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity.		Apoptosis , c-Met/HGFR
T5555	Siremadlin	NVP-HDM 201	E1/E2/E3 Enzyme
	Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.		E1/E2/E3 Enzyme
T11444	GNF-6231		Porcupine
	GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.		Porcupine
T1961	Vistusertib	AZD2014	Apoptosis , Akt , PI3K , S6 Kinase , mTOR , Autophagy
	Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.		Apoptosis , Akt , PI3K , S6 Kinase , mTOR , Autophagy
T6044	Telotristat Etiprate	LX1606 (Hippurate),LX 1606 Hippurate	Hydroxylase
	Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.		Hydroxylase
TQ0086	AF38469	AF-38469	Neurotensin Receptor
	AF38469 is a new, specific and orally bioavailable Sortilin inhibitor (IC50: 330 nM).		Neurotensin Receptor

Compounds

ARD-2128

T39695

Synonym:

Target: Androgen Receptor

Niraparib tosylate monohyrate

Target: Tyrosine Kinases, JAK

Synonym: NS-018 maleate

Target: Tyrosine Kinases, JAK

Ilginatinib hydrochloride

T12266L2

Synonym: NS-018 hydrochloride

Target: Tyrosine Kinases, JAK

GSK-25

T4488

Synonym: GSK25

Target: ROCK, S6 Kinase, mTOR

Niraparib

T3231

Synonym: MK-4827

Target: Apoptosis, Others, PARP

URB-597

T6714

Synonym: KDS-4103,FAAH Inhibitor II

Target: Mitophagy, FAAH, Autophagy

Oprozomib

T6041

Synonym: PR-047,ONX 0912

Target: Proteasome, Autophagy

Venetoclax

T2119

Synonym: GDC-0199,ABT 199,ABT-199,ABT199

Target: BCL, Autophagy

Vercirnon

T17225

Synonym: CCX282-B,GSK-1605786,Traficet-EN

Target: CCR

ms48107

T9146

Synonym: Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-

Target: Others

Niraparib hydrochloride

T3353

Synonym: MK-4827 hydrochloride,MK-4827 (hydrochloride)

Target: Apoptosis, Others, PARP

Niraparib tosylate

T6892

Synonym: MK-4827 (tosylate),MK 4827 tosylate,Niraparib (MK-4827) tosylate

Target: Apoptosis, PARP

Synonym: A-002,LY333013

Target: Others, Phospholipase

AMG2850

T10300

Synonym:

Target: TRP/TRPV Channel

Target: 5-HT Receptor

Target: Apoptosis, Epigenetic Reader Domain

Target: Epigenetic Reader Domain, Histone Methyltransferase

Tulrampator

T17179

Synonym: CX-1632,S-47445

Synonym: NSC12971,NSC 12971,NSC-12971

Target: Phosphatase, Others

Baricitinib phosphate

T2360

Synonym: Baricitinib Phosphate,LY3009104,INCB-028050 phosphate,LY-3009104 phosphate,INCB028050

Target: Tyrosine Kinases, JAK

Synonym: TAK733,TAK 733

Target: Sodium Channel

Silmitasertib

T2259

Synonym: CX-4945

Target: Casein Kinase, Autophagy

Synonym: RG-7112,RG 7112,RO5045337

Target: Mdm2, E1/E2/E3 Enzyme

Synonym: EC D-3263 HCl,D3263 HCl salt

Target: TRP/TRPV Channel

Turofexorate Isopropyl

T6053

Synonym: XL335,FXR-450,WAY-362450

Target: FXR, Autophagy

PF-06882961

T12431

Synonym:

Target: Glucagon Receptor

Tivantinib

T6117

Synonym: ARQ 197

Target: Apoptosis, c-Met/HGFR

Siremadlin

T5555

Synonym: NVP-HDM 201

Target: E1/E2/E3 Enzyme

Target: Apoptosis, Akt, PI3K, S6 Kinase, mTOR, Autophagy

Telotristat Etiprate

T6044

Synonym: LX1606 (Hippurate),LX 1606 Hippurate

Target: Neurotensin Receptor

カタログ番号	製品名	別名	ターゲット
T2807	Caffeic Acid		Lipoxygenase , Endogenous Metabolite , TRP/TRPV Channel
	Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.		Lipoxygenase , Endogenous Metabolite , TRP/TRPV Channel
T13092	Tauro-Obeticholic acid		FXR
	Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).		FXR
T5041	Faropenem sodium		Antibacterial , Antibiotic
	Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.It treatment of tuberculosis and community-acquired pneumonia.		Antibacterial , Antibiotic
T5113	L-GLUCOSE	L-(-)-Glucose	Others
	L-Glucose (L-(-)-Glucose) is an enantiomer of D-glucose. L-Glucose is not bioavailable to cells as an energy source because it cannot be phosphorylated by hexokinase.		Others
T6674	L-Ascorbic acid sodium salt	(+)-Sodium L-ascorbate,Vitamin C sodium salt,Sodium ascorbate,L-Ascorbic acid sodium,Sodium L-ascorbate	Apoptosis , Others , Calcium Channel , Reactive Oxygen Species , Endogenous Metabolite
	L-Ascorbic acid sodium salt (Vitamin C sodium salt) is a more bioavailable form of vitamin C that is an alternative to taking ascorbic acid as a supplement.
T2220	2-Methoxyestradiol	NSC-659853,2-MeOE2,2-ME2	Apoptosis , Reactive Oxygen Species , Microtubule Associated , Endogenous Metabolite , HIF , Autophagy
	2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endotheli...
T6491	(-)-(S)-Equol	(−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol	Estrogen Receptor/ERR , Estrogen/progestogen Receptor , Endogenous Metabolite
	(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective a...