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Search Result

Search Results for " allosteric "

Targets

cAMP Cannabinoid Receptor

615

Compounds

11

Natural Products

11

Recombinant Proteins

2

Libraries

Cat No. Product Name Synonyms Targets
T61562 CB1R Allosteric modulator 3 cAMP , Cannabinoid Receptor
CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction.
T5456 WNK-IN-11 Allosteric WNK Kinase Inhibitor Serine/threonin kinase
WNK-IN-11 (Allosteric WNK Kinase Inhibitor) is an allosteric With-No-Lysine (WNK) kinase inhibitor,WNK1(IC50 : 4 nM)
T62016 CB1R Allosteric modulator 1
CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
T61276 CB1R Allosteric modulator 2
CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previo...
T61371 CB1R Allosteric modulator 4
CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arresti...
T64096 Integrase-LEDGF/p75 allosteric inhibitor 1
Integrase-LEDGF/p75 allosteric inhibitor 1 is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. It inhibits HIV-1 DNA integration and exhibits antiviral effects, acting on the HIV-1 recombinant mo...
T22641 CDPPB GluR
CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).
T21781 A-286982 Integrin
A 286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.
T3464 PHCCC (-) PHCCC GluR
PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8.
T22703 CYM-5520 CYM 5520 S1P Receptor , LPL Receptor
CYM-5520 is a noncompetitive allosteric agonist of S1P2
T8868 4BP-TQS AChR
4BP-TQS is an allosteric agonist of α7 nAChRs.
T9884 EN523 Others
EN523 targets non-catalytic allosteric cysteine C23 in K48 ubiquitin-specific deuquitinase OTUB1.
T4573 Cyclothiazide GluR
Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).
T23515 VU-29 VU 29 GluR
VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
T21747 VU0483605 GluR
VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.
T22027 AH-7614 AH 7614 GPR
AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.
T9238 KI-7 Adenosine Receptor
KI-7 is an adenosine A2B receptor positive allosteric modulator.
T22711 DCB 3,3'-dichlorobenzaldazine Others , GluR
DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of ...
T8642 4-CMTB GPR
4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).
T9466 RTICBM-189 Others
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel...
T26869 BMS-986122 BMS 986122 Opioid Receptor
BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC5...
T23513 VU10010 VU 10010 AChR
VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.
T9699 TAK-615 LPA Receptor
TAK-615 is commonly used to study pulmonary fibrosis and is a negative allosteric modulator of LPA1 receptors.
T14127 Adenosine A1 receptor activator T62 Adenosine Receptor
Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor, and it produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve...
T28069 ML380 ML 380,ML-380 AChR
ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).
T12103 MR-L2 PDE
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).
T15050 Danicamtiv MYK-491,SAR 440181 Myosin
Danicamtiv (MYK-491) is an inotropic agent and it also is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
T29137 VU0453595 VU 0453595,VU-0453595 AChR
VU0453595 is a M1 positive allosteric modulator (PAM).
T36670 JNJ-67856633 MALT
JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric inhibitor of MALT1 protease . JNJ-67856633 lead to tumor stasis in some cases.
T0830 Bithionol Actamer cAMP , Parasite
Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bit...
T8497 SX-682 CXCR
SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.
T7776 ADH-503 GB1275 Complement System
ADH-503 (GB1275) is a potent agonist of the integrin CD11b to mitigate myeloid cell immunosuppression.
T9694 Emraclidine CVL-231 AChR
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator and can be used in neurological diseases studies.
T8776 FEMA 4774 S9632 Others
FEMA 4774 (S9632) is a positive allosteric modulator of T1R2/T1R3. FEMA4774 shows obvious enhancement of the sweetness of sucrose in sensory evaluation tests
T13176 TNO155 Batoprotafib Phosphatase
TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.
T22282 Brr2-IN-3 Brr2 Inhibitor 9,Brr2 Inhibitor C9 Others
Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).
T2463 ML141 CID-2950007 Apoptosis , CDK , Ras
ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).
T4190 Ticlopidine PCR 5332,Ticlid ATPase , Adiponectin receptor
Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.
T10826 CK-666 HIV Protease , Microtubule Associated
CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex. It binds to the Arp2/3 complex, stabilizes the inactive state of the complex, blocking the movement of the Arp2 and Arp3 subunits into the act...
T23469 TQS 4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide AChR
TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.
T9072 Tuxobertinib BDTX-189 EGFR , HER , BTK , RIP kinase
Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activ...
T1817 GNF-2 GNF2 SARS-CoV , Bcr-Abl
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
T8421 TED-347 YAP
TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.
T26396 6-Hydroxy-DOPA 6-Hydroxy-DL-DOPA DNA/RNA Synthesis
6-Hydroxy-DOPA is an allosteric inhibitor of RAD52, it inhibits proliferation of BRCA-deficient cancer cells in vitro and also inhibits APE1.
T21935L AMN082 free base AMN082 GluR
AMN082 free base is a metabotropic glutamate receptor 7 allosteric agonist.
T8872 (Rac)-JBJ-04-125-02 JBJ-04-125-02 EGFR
(Rac)-JBJ-04-125-02 (JBJ-04-125-02) is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer.
T23008L MMPIP hydrochloride MMPIP hydrochloride (479077-02-6 Free base) GluR
MMPIP hydrochloride is a selective antagonist of allosteric mGluR7. MMPIP hydrochloride can be used in research on the roles of mGluR7 on central nervous system functions.
T23524 W-84 dibromide HDMPPA AChR
W-84 dibromide (HDMPPA) is a M2-receptor selective modulator.
T7706 LY-404187 GluR , iGluR
LY404187 is a positive allosteric modulator of AMPA receptors
T7165 Basmisanil RG1662,RO5186582 GABA Receptor
Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndro...

Compounds

CB1R Allosteric modulator 3
T61562
Synonym:
Target: cAMP, Cannabinoid Receptor
WNK-IN-11
T5456
Synonym: Allosteric WNK Kinase Inhibitor
Target: Serine/threonin kinase
CB1R Allosteric modulator 1
T62016
Synonym:
Target:
CB1R Allosteric modulator 2
T61276
Synonym:
Target:
CB1R Allosteric modulator 4
T61371
Synonym:
Target:
Integrase-LEDGF/p75 allosteric inhibitor 1
T64096
Synonym:
Target:
CDPPB
T22641
Synonym:
Target: GluR
A-286982
T21781
Synonym:
Target: Integrin
PHCCC
T3464
Synonym: (-) PHCCC
Target: GluR
CYM-5520
T22703
Synonym: CYM 5520
Target: S1P Receptor, LPL Receptor
4BP-TQS
T8868
Synonym:
Target: AChR
EN523
T9884
Synonym:
Target: Others
Cyclothiazide
T4573
Synonym:
Target: GluR
VU-29
T23515
Synonym: VU 29
Target: GluR
VU0483605
T21747
Synonym:
Target: GluR
AH-7614
T22027
Synonym: AH 7614
Target: GPR
KI-7
T9238
Synonym:
Target: Adenosine Receptor
DCB
T22711
Synonym: 3,3'-dichlorobenzaldazine
Target: Others, GluR
4-CMTB
T8642
Synonym:
Target: GPR
RTICBM-189
T9466
Synonym:
Target: Others
BMS-986122
T26869
Synonym: BMS 986122
Target: Opioid Receptor
VU10010
T23513
Synonym: VU 10010
Target: AChR
TAK-615
T9699
Synonym:
Target: LPA Receptor
Adenosine A1 receptor activator T62
T14127
Synonym:
Target: Adenosine Receptor
ML380
T28069
Synonym: ML 380,ML-380
Target: AChR
MR-L2
T12103
Synonym:
Target: PDE
Danicamtiv
T15050
Synonym: MYK-491,SAR 440181
Target: Myosin
VU0453595
T29137
Synonym: VU 0453595,VU-0453595
Target: AChR
JNJ-67856633
T36670
Synonym:
Target: MALT
Bithionol
T0830
Synonym: Actamer
Target: cAMP, Parasite
SX-682
T8497
Synonym:
Target: CXCR
ADH-503
T7776
Synonym: GB1275
Target: Complement System
Emraclidine
T9694
Synonym: CVL-231
Target: AChR
FEMA 4774
T8776
Synonym: S9632
Target: Others
TNO155
T13176
Synonym: Batoprotafib
Target: Phosphatase
Brr2-IN-3
T22282
Synonym: Brr2 Inhibitor 9,Brr2 Inhibitor C9
Target: Others
ML141
T2463
Synonym: CID-2950007
Target: Apoptosis, CDK, Ras
Ticlopidine
T4190
Synonym: PCR 5332,Ticlid
Target: ATPase, Adiponectin receptor
CK-666
T10826
Synonym:
Target: HIV Protease, Microtubule Associated
TQS
T23469
Synonym: 4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide
Target: AChR
Tuxobertinib
T9072
Synonym: BDTX-189
Target: EGFR, HER, BTK, RIP kinase
GNF-2
T1817
Synonym: GNF2
Target: SARS-CoV, Bcr-Abl
TED-347
T8421
Synonym:
Target: YAP
6-Hydroxy-DOPA
T26396
Synonym: 6-Hydroxy-DL-DOPA
Target: DNA/RNA Synthesis
AMN082 free base
T21935L
Synonym: AMN082
Target: GluR
(Rac)-JBJ-04-125-02
T8872
Synonym: JBJ-04-125-02
Target: EGFR
MMPIP hydrochloride
T23008L
Synonym: MMPIP hydrochloride (479077-02-6 Free base)
Target: GluR
W-84 dibromide
T23524
Synonym: HDMPPA
Target: AChR
LY-404187
T7706
Synonym:
Target: GluR, iGluR
Basmisanil
T7165
Synonym: RG1662,RO5186582
Target: GABA Receptor
1 2 3 4 5 6 7 8 9 10 11 12 13
Cat No. Product Name Synonyms Targets
T4S0878 Prunetin Prunusetin ERK , Dehydrogenase , NF-κB
1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity/adipogenesis effects by suppressing obesit...
T10085 20(S)-Hydroxycholesterol 20α-Hydroxycholesterol Smo
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo).
T8363 DL-Serine PKM
DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.
T0086 Galanthamine hydrobromide Galantamine hydrobromide,Galanthamine HBr AChR , AChE
Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.
T3318 Wogonoside Glychionide B,Wogonin 7-O-glucuronide,Oroxindin GABA Receptor , Autophagy
Wogonoside (Wogonin 7-O-glucuronide) acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.
TN3174 6-Methoxyflavanone NSC50184 GABA Receptor
6-Methoxyflavanone (6-MeOF) is A positive allosteric modulator of the GABA response of human recombinant GABA A receptor, with antianxiety and anti-inflammatory activity, and can be used to reduce cisplatin induced neuro...
TN1325 (2S)-6-Prenylnaringenin 6-Prenylnaringenin,6-PN GABA Receptor
(2S)-6-Prenylnaringenin (6-Prenylnaringenin) is an isomer of the potent phytoestrogen, 8-prenylnaringenin. (2S)-6-Prenylnaringenin is the most potent compound in the forebrain and acts as a positive allosteric modulator ...
T0069 Uracil Others , Endogenous Metabolite
Uracil is a common naturally occurring pyrimidine found in RNA, it base pairs with adenine and is replaced by thymine in DNA. Methylation of uracil produces thymine. Uracil's use in the body is to help carry out the synt...
T2946 Tanshinone IIA sulfonate sodium Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium CaMK , P450 , Calcium Channel
Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor...
T10609 Brevetoxin-3 PbTx-3 Others
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator. Brevetoxin-3 has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels.
T71795 Norstictic acid
Norstictic acid is a potent, selective allosteric transcriptional regulator that exhibits anticancer, antioxidant, and antimicrobial activities.

Natural Products

Prunetin
T4S0878
Synonym: Prunusetin
Target: ERK, Dehydrogenase, NF-κB
20(S)-Hydroxycholesterol
T10085
Synonym: 20α-Hydroxycholesterol
Target: Smo
DL-Serine
T8363
Synonym:
Target: PKM
Galanthamine hydrobromide
T0086
Synonym: Galantamine hydrobromide,Galanthamine HBr
Target: AChR, AChE
Wogonoside
T3318
Synonym: Glychionide B,Wogonin 7-O-glucuronide,Oroxindin
Target: GABA Receptor, Autophagy
6-Methoxyflavanone
TN3174
Synonym: NSC50184
Target: GABA Receptor
(2S)-6-Prenylnaringenin
TN1325
Synonym: 6-Prenylnaringenin,6-PN
Target: GABA Receptor
Uracil
T0069
Synonym:
Target: Others, Endogenous Metabolite
Tanshinone IIA sulfonate sodium
T2946
Synonym: Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium
Target: CaMK, P450, Calcium Channel
Brevetoxin-3
T10609
Synonym: PbTx-3
Target: Others
Norstictic acid
T71795
Synonym:
Target:

Recombinant Proteins

Species：
Human (8)
Mouse (3)
Expression System：
E. coli (6)
Baculovirus-Insect Cells (4)
Yeast (1)
Tag：
His (3)
His,GST (3)
N-terminal 6xHis-tagged (3)
N-6His (1)
N-terminal 10xHis-tagged (1)
Cat No. Product Name Species Expression System
TMPY-02707 PAH Protein, Human, Recombinant (415 Asn/Asp, His) Human Baculovirus-Insect Cells
PAH (phenylalanine hydroxylase), also known as PH, belongs to the biopterin-dependent aromatic amino acid hydroxylase family. It contains 1 ACT domain, N-terminal region of PAH is thought to contain allosteric binding si...
TMPH-01266 RNF13 Protein, Human, Recombinant (His) Human E. coli
TMPY-04474 PFKFB3 Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
Fructose-2,6-biphosphatase 3, also known as 6-phosphofructo-2-kinase or PFK2 or PFKFB3, is a potent activator of phosphofructokinase, which is a rate-limiting enzyme of glycolysis. Highly phosphorylated PFKFB3 protein wa...
TMPY-03868 ARF5 Protein, Human, Recombinant (His) Human E. coli
ARF5, also known as ADP-ribosylation factor 5, belongs to the small GTPase superfamily, Arf family. Members of this family stimulate the ADP-ribosyltransferase activity of cholera toxin and play a role in vesicular traff...
TMPY-03796 ARF3 Protein, Human, Recombinant (His) Human E. coli
ARF3, also known as ADP-ribosylation factor 3, belongs to the RAS superfamily. Members of this family include ARF1, ARF2, ARF3, ARF4, ARF5 and ARF6. ARF3 gene is a member of the human ARF gene family. These genes encode ...
TMPY-02379 EED Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
EED is essential for regulating the repressive histone modification, histone 3 lysine 27 tri-methylation (H3K27me3) at many developmental genes. EED depletion significantly impeded erythroid maturation. EED depletion imp...
TMPY-04462 HK3 Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
Hexokinase-3, also known as Hexokinase type III, HKIII, and HK3, is a protein that belongs to the hexokinase family. Hexokinase-3 / HK3 is an enzyme that in humans is encoded by the HK2 gene. Hexokinases phosphorylate gl...
TMPJ-01055 HBA1 Protein, Human, Recombinant (His) Human E. coli
Hemoglobin subunit alpha 1 (HBA1), also known as α2β2, is a hetero-tetramer consisting of two α and two β subunits held together by non-covalent interactions. Each subunit contains a heme group with an iron atom in the F...
TMPH-02481 PRKAG1 Protein, Mouse, Recombinant (His) Mouse E. coli
AMP/ATP-binding subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular ATP levels, AMPK a...
TMPH-02638 HSPA5 Protein, Mouse, Recombinant (E. coli, His) Mouse E. coli
Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its i...
TMPH-02639 HSPA5 Protein, Mouse, Recombinant (His) Mouse Yeast
Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its i...
Cat No. Product Name
L1120 AMPK-Targeted Compound Library

80 compounds
80 well-chosen unique AMPK-targeted small molecules；
L2550 Glutamine Metabolism Compound Library

580 compounds
A unique collection of 580 glutamine metabolism related compounds can be used for high throughput screening (HTS) and high content screening (HCS), and also is an effective tool for research in glutamine metabolism and ...

Libraries

AMPK-Targeted Compound Library
L1120
Compounds: 80
Glutamine Metabolism Compound Library
L2550
Compounds: 580
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