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binding-site

" in MedChemExpress (MCE) Product Catalog:

277

Inhibitors & Agonists

6

Screening Libraries

6

Fluorescent Dye

2

Biochemical Assay Reagents

37

Peptides

1

MCE Kits

2

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18

Natural
Products

23

Isotope-Labeled Compounds

2

Click Chemistry

2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N7433
    4,6-O-Ethylidene-α-D-glucose

    Ethylidene-glucose

    		 GLUT Endogenous Metabolite Metabolic Disease
    4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport .
    4,6-O-Ethylidene-α-D-glucose
  • HY-18601
    (±)-BI-D
    5 Publications Verification

    		 HIV HIV Integrase Infection
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
    (±)-BI-D
  • HY-163097
    ZCAN262

    		iGluR Neurological Disease
    ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site .
    ZCAN262
  • HY-16307
    MB05032
    5 Publications Verification

    		 FBPase Metabolic Disease
    MB05032 is a special and efficacious gluconeogenesis inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.
    MB05032
  • HY-162659
    β2AR ligand 1

    		Adrenergic Receptor Others
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS) .
    β2AR ligand 1
  • HY-N7437
    Akuammidine

    		Opioid Receptor DNA/RNA Synthesis Neurological Disease Inflammation/Immunology
    Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties .
    Akuammidine
  • HY-103172
    8-Aminoadenine

    		nAChR Metabolic Disease
    8-Aminoadenine is an adenine receptor ligand, with a Ki of 6.51 μM at the human binding site .
    8-Aminoadenine
  • HY-161800
    Aminoacyl tRNA synthetase-IN-3

    		Aminoacyl-tRNA Synthetase Infection
    Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
    Aminoacyl tRNA synthetase-IN-3
  • HY-P5343
    p53 CBS

    p53 Consensus binding sequence

    		 MDM-2/p53 Others
    p53 CBS (p53 Consensus binding sequence) is a biological active peptide. (p53 consensus DNA binding site)
    p53 CBS
  • HY-B0149S
    Tranexamic acid-d2

    		Isotope-Labeled Compounds Cardiovascular Disease
    Tranexamic acid-d2 is the deuterium labeled Tranexamic acid. Tranexamic acid (Transamin) is an antifibrinolytic for blocking lysine-binding sites of plasmin and elastase-derived plasminogen fragments.
    Tranexamic acid-d2
  • HY-N3269
    Methyl p-hydroxyphenyllactate

    		Others Others
    Methyl p-hydroxyphenyllactate (MeHPLA) is an important cell growth-regulating agent which binds to nuclear type II binding sites in normal and malignant cells .
    Methyl p-hydroxyphenyllactate
  • HY-119453
    Oxycinchophen

    		Others Metabolic Disease Inflammation/Immunology
    Oxycinchophen exhibits anti-inflammatory and uricosuric activity. Oxycinchophen displaces urate from albumin, exhibits high affinity for the DNSA-binding site on the albumin molecule .
    Oxycinchophen
  • HY-B0115
    Pizotifen
    2 Publications Verification

    Pizotyline; BC-105

    		 5-HT Receptor Neurological Disease
    Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen
  • HY-107578
    Macbecin

    Macbecin I; NSC 330499

    		 HSP Cancer
    Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities .
    Macbecin
  • HY-118251
    PD130883

    		Antifolate Dihydrofolate reductase (DHFR) Cancer
    PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
    PD130883
  • HY-156871
    CAMK1D-IN-1

    		Others Others
    CAMK1D-IN-1 is a potent inhibitor that targets the ATP-binding site of GSK-3, functioning as a GSK-3 inhibitor.
    CAMK1D-IN-1
  • HY-100982
    (E)-4-Hydroxycrotonic acid

    trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA

    		 Others Neurological Disease
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
    (E)-4-Hydroxycrotonic acid
  • HY-136280
    Panamesine

    EMD 57445

    		 Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-D0871
    CHES

    N-Cyclohexyltaurine

    		 Biochemical Assay Reagents Others Cancer
    CHES (N-Cyclohexyltaurine) is a zwitterionic buffer. CHES can bind to hemagglutinin (HA) emulating with sialic acid (SA) and receptor binding site (RBS)-targeting broadly neutralizing antibodies .
    CHES
  • HY-129927
    Thiomuscimol

    		Others Others
    Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
    Thiomuscimol
  • HY-B0115A
    Pizotifen malate
    2 Publications Verification

    Pizotyline malate; BC-105 malate

    		 5-HT Receptor Neurological Disease
    Pizotifen malate (Pizotyline malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen malate
  • HY-P0186
    Endomorphin 2

    		Opioid Receptor Neurological Disease
    Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2
  • HY-D1030
    Fluorescein Biotin

    		Fluorescent Dye Inflammation/Immunology
    Fluorescein Biotin is used as an alternative to radioactive biotin for detecting and quantitating biotin-binding sites by either fluorescence or absorbance; the the fluorescence or absorbance of Fluorescein Biotin is quenched, upon binding to avidin or streptavidin.
    Fluorescein Biotin
  • HY-D0987
    Stains-All

    		Calmodulin Others
    Stains-All, a cationic carbocyanine dye, is a convenient probe to study the structural features of the individual calcium-binding sites of calmodulin (CaM) and related calcium-binding proteins (CaBP) .
    Stains-All
  • HY-100815B
    (RS)-AMPA

    (±)-AMPA

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA
  • HY-100815D
    (RS)-AMPA monohydrate

    (±)-AMPA monohydrate

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA monohydrate
  • HY-125956
    Aurkin A

    		Aurora Kinase Cancer
    Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM .
    Aurkin A
  • HY-124673
    AF40431
    1 Publications Verification

    		 Neurotensin Receptor Neurological Disease
    AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 µM and a Kd of 0.7 µM . AF40431 is bound in the neurotensin-binding site of sortilin .
    AF40431
  • HY-152156
    Tubulin inhibitor 11

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
    Tubulin inhibitor 11
  • HY-157543
    Tubulin polymerization-IN-59

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-59 ((R)-9k) is a potent inhibitor of colchicine binding site inhibitor (CBSI). Tubulin polymerization-IN-59 inhibits tubulin polymerization .
    Tubulin polymerization-IN-59
  • HY-100815E
    (RS)-AMPA hydrochloride

    (±)-AMPA hydrochloride

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) hydrochloride is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA hydrochloride
  • HY-P0186A
    Endomorphin 2 TFA

    		Opioid Receptor Neurological Disease
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
    Endomorphin 2 TFA
  • HY-131941
    SJM-3

    		GABA Receptor Neurological Disease
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
    SJM-3
  • HY-100815C
    (RS)-AMPA hydrobromide

    (±)-AMPA hydrobromide

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA hydrobromide
  • HY-119581
    MBED

    9-Methyl-7-bromoeudistomin D

    		 Others Neurological Disease
    MBED (9-Methyl-7-bromoeudistomin D) is a RyR agonist. MBED is a high-affinity caffeine-like probe, helps identify the caffeine-binding site in RyRs .
    MBED
  • HY-123708
    SNAP 398299

    		Others Others
    SNAP 398299 is a compound mentioned in the study of Gal3 receptor inhibitors. Through molecular dynamics simulation and docking studies, it provides a structural basis and understanding of the binding site for the design of more effective inhibitors.
    SNAP 398299
  • HY-119105
    LY81067

    		Others Neurological Disease
    LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites .
    LY81067
  • HY-106825
    Clanfenur

    		Microtubule/Tubulin Cancer
    Clanfenur is a substituted benzoylphenylurea, an analogue of the pesticide fenfluramide, with potential antineoplastic activity. Clanfenur can bind to the colchicine-binding site on β-tubulin, inhibit microtubule polymerization, and thus prevent tumor cell replication .
    Clanfenur
  • HY-100998
    Metaphit

    		Others Neurological Disease
    Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates . Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms .
    Metaphit
  • HY-163746
    BuChE-IN-11

    		Cholinesterase (ChE) Neurological Disease
    BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
    BuChE-IN-11
  • HY-100714A
    D-AP5
    15+ Cited Publications

    D-APV; D-2-Amino-5-phosphonovaleric acid

    		 iGluR Neurological Disease
    D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
    D-AP5
  • HY-151982
    Tubulin polymerization-IN-39

    		Microtubule/Tubulin Cardiovascular Disease Cancer
    Tubulin polymerization-IN-39 is a tubulin polymerization inhibitor (IC50: 4.9 μM). Tubulin polymerization-IN-39 occupies the colchicine-binding site. Tubulin polymerization-IN-39 inhibits cancer cell proliferation .
    Tubulin polymerization-IN-39
  • HY-137974
    8-Epixanthatin

    		STAT Apoptosis Cancer
    8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity .
    8-Epixanthatin
  • HY-153761
    ASK1-IN-4

    		MAP3K Apoptosis Inflammation/Immunology Cancer
    ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1 .
    ASK1-IN-4
  • HY-162594
    Antitumor agent-164

    		Microtubule/Tubulin Cancer
    Antitumor agent-164 (compound 60c) is a colchicine-binding site inhibitor (CBSI) with potency against taxane-sensitive TNBC. Antitumor agent-164 is a next-generation derivative of VERU-111 .
    Antitumor agent-164
  • HY-152143
    Tubulin polymerization-IN-41

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects .
    Tubulin polymerization-IN-41
  • HY-148705
    Isomitomycin A

    		SARS-CoV Infection
    Isomitomycin A is a potential inhibitor against SARS-CoV-2. Isomitomycin A targets to the hACE2 binding site of the modelled surface glycoprotein of SARS-CoV-2. Isomitomycin A can be used in studies of COVID-19 .
    Isomitomycin A
  • HY-155941
    5-Hydroxydecanoic acid

    		Potassium Channel Neurological Disease
    5-Hydroxydecanoic acid (5-HD） is a KATP channel antagonist，which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
    5-Hydroxydecanoic acid
  • HY-P1887
    p5 Ligand for Dnak and DnaJ

    		HSP Infection
    p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ .
    p5 Ligand for Dnak and DnaJ
  • HY-P9963
    Blinatumomab
    1 Publications Verification

    Anatumomab

    		 CD19 Cancer
    Blinatumomab (Anatumomab) is a bispecific monoclonal antibody with two binding sites, one for CD3E on T cells and one for CD19 on B cells. Blinatumomab can be used in research for acute lymphoblastic leukemia .
    Blinatumomab

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