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IC50

  • IC50
  • Half maximal inhibitory concentration

    inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative

    IC50

    IC50

    IC50

  • Keanumycin
  • Group of chemical compounds

    amoebas Dictyostelium discoideum (IC50 = 4.4 nM), Acanthamoeba castellanii (IC50 = 2.0 μM), and Acanthamoeba comandoni (IC50 = 3.1 μM) which cause infections

    Keanumycin

    Keanumycin

  • Tianeptinaline
  • Pharmaceutical compound

    (HDAC1 IC50 = 0.240 µM, HDAC2 IC50 = 0.120 µM, HDAC3 IC50 = 0.155 µM, HDAC5 IC50 > 80 µM, HDAC6 IC50 > 80 µM), such as CI‐994 (3) (HDAC1 IC50 = 0.145

    Tianeptinaline

    Tianeptinaline

    Tianeptinaline

  • Substituted naphthylethylamine
  • Class of chemical compounds

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Substituted naphthylethylamine

    Substituted naphthylethylamine

    Substituted_naphthylethylamine

  • Cyclobenzaprine
  • Muscle relaxant medication

    5HT2a (IC50 = 92 nM) by Ca+ mobilization. CBP is also an antagonist on 5HT2b (IC50 = 100 nM). CBP and nCBP are functional antagonists on 5HT2c (IC50 = 0

    Cyclobenzaprine

    Cyclobenzaprine

    Cyclobenzaprine

  • AEE788
  • Chemical compound

    factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. In cells, growth factor-induced

    AEE788

    AEE788

    AEE788

  • ERAP2
  • Protein-coding gene in the species Homo sapiens

    manner (IC50 = 44 μM) by inhibiting the hydrolysis of peptide substrates. At the same time it acts as a competitive inhibitor against ERAP1 (IC50 = 73 μM)

    ERAP2

    ERAP2

    ERAP2

  • GTx1-15
  • Toxin from the Chilean tarantula venom

    Channels IC50 Cav3.1 0.01 μM Nav1.7 0.007 μM Nav1.3 0.12 ± 0.06 μM Nav1.5 No significant effect (up to 2 μΜ) Nav1.8 No significant effect (0.93 μM)

    GTx1-15

    GTx1-15

  • Phenmetrazine
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Phenmetrazine

    Phenmetrazine

    Phenmetrazine

  • 2-Phenylmorpholine
  • Pharmaceutical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    2-Phenylmorpholine

    2-Phenylmorpholine

    2-Phenylmorpholine

  • MDMAR
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    MDMAR

    MDMAR

    MDMAR

  • List of benzodiazepines
  • agonists (e.g. flumazenil). Low IC50 or high pIC50 values indicate tighter binding (pIC50 of 8.0 = IC50 of 10nM, pIC50 of 9.0 = IC50 of 1nM, etc.) These are non

    List of benzodiazepines

    List of benzodiazepines

    List_of_benzodiazepines

  • Intercity (Deutsche Bahn)
  • Locomotive-hauled long-distance passenger rail service in Germany

    Intercity, often shortened to IC ([iːˈtseː] ), is the second-highest train classification in Germany, after the Intercity Express (ICE). Intercity services

    Intercity (Deutsche Bahn)

    Intercity (Deutsche Bahn)

    Intercity_(Deutsche_Bahn)

  • 4-Methylmethamphetamine
  • Stimulant and entactogen drug of the amphetamine class

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    4-Methylmethamphetamine

    4-Methylmethamphetamine

    4-Methylmethamphetamine

  • SR9009
  • Chemica compound, Agonist of Rev-ErbA

    Rev-ErbA) with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ. In an animal study, some of its

    SR9009

    SR9009

    SR9009

  • Aminorex
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Aminorex

    Aminorex

    Aminorex

  • 1-Naphthylaminopropane
  • Pharmaceutical compound

    of MAO-A (IC50 = 5,630 nM), but was about 13-fold less potent than 2-NAP. Neither 2-NAP or 1-NAP inhibited monoamine oxidase B (MAO-B) (IC50 > 100,000 nM)

    1-Naphthylaminopropane

    1-Naphthylaminopropane

    1-Naphthylaminopropane

  • GSK-3
  • Class of enzymes

    (IC50=7.5μM) TDZD-8 (IC50=2μM) NP00111 (IC50=2μM) NP031115 (IC50=4μM) Tideglusib (IC50=60nM) HMK-32 (IC50=1.5μM) L803-mts (IC50=20μM) L807-mts (IC50=1μM)

    GSK-3

    GSK-3

    GSK-3

  • GYKI 52466
  • Chemical compound

    receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA-, kainate- and NMDA-induced

    GYKI 52466

    GYKI 52466

    GYKI_52466

  • Phentermine
  • Weight loss medication

    of potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). [...] Chlorphentermine was a very potent 5-HT releaser (IC50 = 18.2 nM), a weaker

    Phentermine

    Phentermine

    Phentermine

  • SR9011
  • Chemical compound

    Rev-ErbAα with a half-maximum inhibitory concentration (IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ. It has been used in the study of

    SR9011

    SR9011

    SR9011

  • Phenylpiracetam
  • Chemical compound

    of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)

    Phenylpiracetam

    Phenylpiracetam

    Phenylpiracetam

  • Canertinib
  • Chemical compound

    tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). By 2015, Pfizer had discontinued development

    Canertinib

    Canertinib

    Canertinib

  • Β-Carboline
  • Group of chemical compounds

    of 1,700 nM. It is also a weak dopamine reuptake inhibitor (DRI), with an IC50 of 3,040 nM at the dopamine transporter (DAT). The drug shows weak affinity

    Β-Carboline

    Β-Carboline

    Β-Carboline

  • Hydroxychavicol
  • Chemical compound

    leaves of Piper betle. It is a more potent inhibitor of xanthine oxidase (IC50=16.7 μM) than allopurinol. It might be a useful new compound in treating

    Hydroxychavicol

    Hydroxychavicol

    Hydroxychavicol

  • MDPHP
  • Chemical compound

    MDPHP acts as a potent norepinephrine-dopamine reuptake inhibitor. The IC50 values for MDPHP are 60-935 nM at NET, 8.4-50 nM at DAT and 9000 nM at SERT

    MDPHP

    MDPHP

    MDPHP

  • Tesofensine
  • Chemical compound

    Tesofensine has IC50 of 8.0, 3.2 and 11.0nM at the DAT, NET, and SERT. More recently, though, the following data was submitted: IC50 (nM) NET 1.7, SERT

    Tesofensine

    Tesofensine

    Tesofensine

  • Memantine
  • Medication used to treat Alzheimer's disease

    antagonist, with an IC50 binding affinity of ~500-1,000 nM (0.5-1 μM), but displays higher potency at extrasynaptic NMDA receptors (IC50 = ~22 nM), suggesting

    Memantine

    Memantine

    Memantine

  • 4-Nonylphenylboronic acid
  • Chemical compound

    hydrolase (FAAH), with an IC50 of 9.1nM, and 870x selectivity for FAAH over the related enzyme MAGL, which it inhibits with an IC50 of 7900nM. It is also

    4-Nonylphenylboronic acid

    4-Nonylphenylboronic_acid

  • 2-Benzylpiperidine
  • Chemical compound

    transporter (DAT) has been reported to be 6,360 nM and its functional inhibition (IC50) of the DAT has been reported to be 3,780 to 8,800 nM. These values were

    2-Benzylpiperidine

    2-Benzylpiperidine

    2-Benzylpiperidine

  • 4-Methylaminorex
  • Group of stereoisomers

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    4-Methylaminorex

    4-Methylaminorex

    4-Methylaminorex

  • Discovery and development of gliflozins
  • Drug discovery

    n-pentyl group (IC50 = 13,3 nM), n-butyl (IC50 = 119 nM), phenyl with 2-furyl (IC50 = 0,720) or 3-thiophenyl (IC50 = 0,772). As seen in table 1, the in vitro

    Discovery and development of gliflozins

    Discovery_and_development_of_gliflozins

  • PDBbind database
  • collection of experimentally measured binding affinity data (Kd, Ki, and IC50) for the protein-ligand complexes deposited in the Protein Data Bank (PDB)

    PDBbind database

    PDBbind_database

  • RU-27849
  • Pharmaceutical compound

    have much higher affinity for serotonin receptors than RU-27849 itself (IC50 ≈ 50 nM). A number of other derivatives also exist, including FHATHBIN (6-hydroxy)

    RU-27849

    RU-27849

    RU-27849

  • 4-Methylamphetamine
  • Stimulant and anorectic drug of the amphetamine class

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    4-Methylamphetamine

    4-Methylamphetamine

    4-Methylamphetamine

  • Fedratinib
  • Chemical compound

    inhibitor of protein kinase JAK-2 with IC50=6 nM; related kinases FLT3 and RET are also sensitive, with IC50=25 nM and IC50=17 nM, respectively. Significantly

    Fedratinib

    Fedratinib

    Fedratinib

  • Naphthylaminopropane
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Naphthylaminopropane

    Naphthylaminopropane

    Naphthylaminopropane

  • Naphthylmetrazine
  • Pharmaceutical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Naphthylmetrazine

    Naphthylmetrazine

    Naphthylmetrazine

  • CDD-2807
  • Chemical compound

    selective inhibitor of serine/threonine-protein kinase 33 (STK33), with a IC50 of 9.2 nM. In animal studies it causes production of abnormal sperm with

    CDD-2807

    CDD-2807

    CDD-2807

  • 2-Naphthylmethcathinone
  • Substituted cathinone stimulant drug

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    2-Naphthylmethcathinone

    2-Naphthylmethcathinone

    2-Naphthylmethcathinone

  • EC50
  • Concentration of a compound where 50% of its maximal effect is observed

    (x axis). For competition binding assays and functional antagonist assays IC50 is the most common summary measure of the dose-response curve. For agonist/stimulator

    EC50

    EC50

    EC50

  • Hydroxyflutamide
  • Chemical compound

    hydroxyflutamide as the active form. It has been reported to possess an IC50 of 700 nM for the androgen receptor (AR), which is about 4-fold less than

    Hydroxyflutamide

    Hydroxyflutamide

    Hydroxyflutamide

  • Methamnetamine
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Methamnetamine

    Methamnetamine

    Methamnetamine

  • Dehydronorketamine
  • Chemical compound

    negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 = 55 nM). For this reason, similarly to hydroxynorketamine (HNK), it has

    Dehydronorketamine

    Dehydronorketamine

    Dehydronorketamine

  • Racetam
  • Class of drugs

    of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)

    Racetam

    Racetam

  • Hornet
  • Genus of eusocial wasp

    its IC50 was nearly 128 μL, so we confirmed that LDH absorbance was not affected by this peptide." p. 262, "Moreover, the results showed the IC50 of mast

    Hornet

    Hornet

    Hornet

  • APICA (synthetic cannabinoid drug)
  • Chemical compound

    testing determined APICA to have an IC50 of 175 nM at CB1, only slightly less potent than JWH-018 which had an IC50 of 169 nM, but over four times more

    APICA (synthetic cannabinoid drug)

    APICA (synthetic cannabinoid drug)

    APICA_(synthetic_cannabinoid_drug)

  • Ligand (biochemistry)
  • Substance that forms a complex with a biomolecule

    the receptor. Ligand affinities are most often measured indirectly as an IC50 value from a competition binding experiment where the concentration of a

    Ligand (biochemistry)

    Ligand (biochemistry)

    Ligand_(biochemistry)

  • Ligand efficiency
  • Measure of a ligand's binding energy per atom

    non-hydrogen atoms. It can be transformed to the equation: LE = 1.4(−log IC50)/N Some suggest that better metrics for ligand efficiency are percentage/potency

    Ligand efficiency

    Ligand_efficiency

  • Pseudophenmetrazine
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Pseudophenmetrazine

    Pseudophenmetrazine

    Pseudophenmetrazine

  • Bupropion
  • Medication mainly used for depression and smoking cessation

    7,600–28,000 IC50 Human α3β2-nACh 1,000 IC50 Human α3β4-nACh 1,800 IC50 Human α4β2-nACh 12,000 IC50 Human α4β4-nACh 12,000–14,000 IC50 Human α7-nACh

    Bupropion

    Bupropion

    Bupropion

  • Harmine
  • Pharmaceutical compound

    concentration = 33–700 nM) and a very weak dopamine reuptake inhibitor (IC50 = 12,000 nM). Conversely, it is not a dopamine transporter (DAT) substrate

    Harmine

    Harmine

    Harmine

  • Carpaine
  • Chemical compound

    Especially, Carpaine possessed significant anti-plasmodial activity in vitro (IC50 of 0.2 μM) and high selectivity towards the parasites. Circulatory effects

    Carpaine

    Carpaine

    Carpaine

  • Receptor antagonist
  • Type of receptor ligand or drug that blocks a biological response

    antagonist is usually defined by its half maximal inhibitory concentration (i.e., IC50 value). This can be calculated for a given antagonist by determining the

    Receptor antagonist

    Receptor antagonist

    Receptor_antagonist

  • Lipophilic efficiency
  • Parameter used in drug design

    defined as the pIC50 (or pEC50) of interest minus the LogP of the compound. LiPE = pIC 50 − log ⁡ P {\displaystyle {\ce {LiPE}}={\ce {pIC50}}-\log P} In

    Lipophilic efficiency

    Lipophilic efficiency

    Lipophilic_efficiency

  • Toludesvenlafaxine
  • SNDRI antidepressant drug

    norepinephrine reuptake, respectively, toludesvenlafaxine has respective in vitro IC50 values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and dopamine

    Toludesvenlafaxine

    Toludesvenlafaxine

    Toludesvenlafaxine

  • 4-Butylresorcinol
  • Chemical compound

    acid, 4-butylresorcinol has been found to be the most powerful inhibitor by IC50, but the mode of inhibition is reversible. 4-Butylresorcinol can be used

    4-Butylresorcinol

    4-Butylresorcinol

    4-Butylresorcinol

  • Xorphanol
  • Opioid analgesic

    lesser extent as a partial agonist of the μ-opioid receptor (Ki = 0.25 nM; IC50 = 3.4 nM; Imax = 29%) with lower relative intrinsic activity and marked antagonistic

    Xorphanol

    Xorphanol

    Xorphanol

  • Andrographolide
  • Chemical compound

    concentration is 25μM, the IC50 of andrographolide for GSK-3β is 5.58±0.40μM. When the substrate concentration is increased to 90μM, the IC50 increases to 37.7μM

    Andrographolide

    Andrographolide

    Andrographolide

  • Relugolix
  • Chemical compound

    hormone receptor (GnRHR), with a half-maximal inhibitory concentration (IC50) of 0.12 nM. A dosage of relugolix of 40 mg once per day has been found to

    Relugolix

    Relugolix

    Relugolix

  • N-Ethylpentylone
  • Substituted cathinone stimulant drug

    inhibitor and dopamine reuptake inhibitor. It binds to transporters with IC50 values of 37 nM (dopamine transporter), 105 nM (norepinephrine transporter)

    N-Ethylpentylone

    N-Ethylpentylone

    N-Ethylpentylone

  • Clavaric acid
  • Chemical compound

    extracts. Clavaric acid is a reversible farnesyltransferase inhibitor with an IC50 of 1.3 μM. Lingham RB, Silverman KC, Jayasuriya H, Kim BM, Amo SE, Wilson

    Clavaric acid

    Clavaric acid

    Clavaric_acid

  • Discovery and development of NS5A inhibitors
  • Drug discovery

    benzimidazole-benzimidazole structure on inhibitory activity Structure Activity X IC50 (nM) Inhibitory activity >44 None >44 None 11 Very weak 1.7 Weak 0.50 Moderate

    Discovery and development of NS5A inhibitors

    Discovery and development of NS5A inhibitors

    Discovery_and_development_of_NS5A_inhibitors

  • 6-APT
  • Chemical compound

    class which acts as a selective serotonin releasing agent (SSRA). It has IC50 values of 121 nM, 6,436 nM, and 3,371 nM for inhibiting the reuptake of serotonin

    6-APT

    6-APT

    6-APT

  • Vilazodone
  • Antidepressant medication

    acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%). It has negligible

    Vilazodone

    Vilazodone

    Vilazodone

  • Modimelanotide
  • Chemical compound

    kidney injury. It acts as a non-selective melanocortin receptor agonist, with IC50 values of 2.9 nM, 1.9 nM, 3.7 nM, and 110 nM at the MC1, MC3, MC4, and MC5

    Modimelanotide

    Modimelanotide

  • 4,4'-Dimethylaminorex
  • Chemical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    4,4'-Dimethylaminorex

    4,4'-Dimethylaminorex

    4,4'-Dimethylaminorex

  • Jingzhaotoxin
  • Protein from Chinese tarantula venom

    disulfide bridges. Jingzhaotoxins can target multiple channels. The following IC50 values have been determined: '*' Only a dissociation constant (Kd) was measured

    Jingzhaotoxin

    Jingzhaotoxin

  • Fruquintinib
  • Medication

    1, 2, 3 inhibitor Fruquintinib was found to inhibit VEGFR2 (KDR) with an IC50 of 25 nmol/L in the Z-lyte assay. The kinase selectivity of fruquintinib

    Fruquintinib

    Fruquintinib

    Fruquintinib

  • Toyocamycin
  • Chemical compound

    cancer cells. It demonstrates a strong inhibitory effect on CDK9, with an IC50 of 79 nM, while showing considerably weaker activity against other cyclin-dependent

    Toyocamycin

    Toyocamycin

    Toyocamycin

  • Wortmannin
  • Chemical compound

    phosphoinositide 3-kinases (PI3Ks). It has an in vitro inhibitory concentration (IC50) of around 5 nM, making it a more potent inhibitor than LY294002, another

    Wortmannin

    Wortmannin

    Wortmannin

  • Histone deacetylase inhibitor
  • Compounds that inhibit histone deacetylases

    manner with a median inhibitory concentration (IC50) of 5.3, 2.4, and 4.5 mM, respectively. The HDAC6 IC50 was much higher (48.5 mM) (Fig. 1E), and βOHB

    Histone deacetylase inhibitor

    Histone_deacetylase_inhibitor

  • Lu 35-138
  • Pharmaceutical compound

    modulator or allosteric inhibitor of the serotonin transporter (SERT), with an IC50 of 43.8 nM in the later study. Lu 35-138 also shows affinity for the α1-adrenergic

    Lu 35-138

    Lu 35-138

    Lu_35-138

  • Sclerotiorin
  • Chemical compound

    Sclerotiorin is an aldose reductase inhibitor (IC50=0.4 μM) as well as a reversible lipoxygenase inhibitor (IC50=4.2 μM). Chidananda, C; Rao, LJ; Sattur, AP

    Sclerotiorin

    Sclerotiorin

    Sclerotiorin

  • AS-19 (drug)
  • Chemical compound

    substance which acts as a potent agonist at the 5-HT7 receptor, with an IC50 of 0.83 nM. It reverses the amnesia induced by drugs such as scopolamine

    AS-19 (drug)

    AS-19 (drug)

    AS-19_(drug)

  • Mifepristone
  • Antiprogestogen and antiglucocorticoid drug

    steroidal antiprogestogen (IC50 = 0.025 nM for the PR), as well as an antiglucocorticoid (IC50 = 2.2 nM for the GR) and antiandrogen (IC50 = 10 nM for the AR)

    Mifepristone

    Mifepristone

    Mifepristone

  • Crenolanib
  • Chemical compound

    crenolanib is toxic at IC50 concentrations of 7 nM and 8 nM, respectively. Crenolanib has been shown to inhibit PDGFRα with an IC50 of 0.4 ng/mL in porcine

    Crenolanib

    Crenolanib

    Crenolanib

  • Perfluorooctanesulfonamide
  • Chemical compound

    it is an extremely potent uncoupler of oxidative phosphorylation with an IC50 of about 1 micromolar (≈500 nanograms per milliliter or parts per billion)

    Perfluorooctanesulfonamide

    Perfluorooctanesulfonamide

    Perfluorooctanesulfonamide

  • Rebeccamycin
  • Chemical compound

    shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 leukemia cells). It is an antineoplastic

    Rebeccamycin

    Rebeccamycin

    Rebeccamycin

  • Silene latifolia
  • Species of flowering plant

    cell line (IC50: 19.25 µg/mL after 24 hours), while the water sub-extract showed activity against the MDA-MB-231 breast cancer cell line (IC50: 15.20 µg/mL)

    Silene latifolia

    Silene latifolia

    Silene_latifolia

  • Mesembrenone
  • Chemical compound

    spectabilis. It can be consumed orally, smoked, or snorted. It is a potent (IC50 < 1 μM) selective inhibitor of the serotonin transporter (SERT) (that is

    Mesembrenone

    Mesembrenone

    Mesembrenone

  • Mebfap
  • Pharmaceutical compound

    benzo[b]furan isostere. The tryptamine IC50 of 38 nM was about 13-fold lower than the benzofuran, which had an IC50 of 500 nM. Nichols DE (2012). "Structure–activity

    Mebfap

    Mebfap

    Mebfap

  • Stichodactyla toxin
  • Protein family

    C-terminal carboxyl is replaced by an amide. ShK-186 blocks Kv1.3 with an IC50 of 69 pM and exhibits the same specificity for Kv1.3 over closely related

    Stichodactyla toxin

    Stichodactyla toxin

    Stichodactyla_toxin

  • Toxic unit
  • Units used in toxicology

    required to cause a given toxicological endpoint (LC50, EC50, IC50). 1TU=LC50 or 1TU=IC50 for inhibition of growth Since the mass or molar based concentrations

    Toxic unit

    Toxic_unit

  • Methylenedioxypyrovalerone
  • Chemical compound

    and 3,349 nM for serotonin in rat brain synaptosomes. Similarly, MDPV's IC50 values for monoamine reuptake inhibition were 10 nM for dopamine, 80 nM for

    Methylenedioxypyrovalerone

    Methylenedioxypyrovalerone

    Methylenedioxypyrovalerone

  • MRZ-9547
  • Pharmaceutical drug

    of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)

    MRZ-9547

    MRZ-9547

    MRZ-9547

  • Cerdulatinib
  • Chemical compound

    development for treatment of hematological malignancies. It has lowest nM IC50 values against TYK2, JAK1, JAK2, JAK3, FMS, and SYK. It is being developed

    Cerdulatinib

    Cerdulatinib

    Cerdulatinib

  • Ethylnaphthylaminopropane
  • Pharmaceutical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Ethylnaphthylaminopropane

    Ethylnaphthylaminopropane

    Ethylnaphthylaminopropane

  • MG132
  • Chemical compound

    which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 μM and prevents β-secretase cleavage. There are several inhibitors that

    MG132

    MG132

    MG132

  • Naphthylmorpholine
  • Pharmaceutical compound

    potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)

    Naphthylmorpholine

    Naphthylmorpholine

    Naphthylmorpholine

  • Mazindol
  • Appetite suppressant

    transporter 0.45–18 (Ki) 0.92–4.9 (IC50) >10,000 (EC50) SERTTooltip Serotonin transporter 39–272 (Ki) 54–94 (IC50) >10,000 (EC50) SERT2Tooltip Serotonin

    Mazindol

    Mazindol

    Mazindol

  • KN-62
  • Chemical compound

    permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMK II) with IC50 of 900nM, charactered by hydrophobicity. KN-62 also potently inhibits the

    KN-62

    KN-62

    KN-62

  • NIBR2130
  • Pharmaceutical compound

    chemokine CXCR3 receptor antagonist, with an affinity (IC50) of 54 nM and an inhibitory potency (IC50) of 18 to 74 nM. Unlike NIBR2130, LSD itself is completely

    NIBR2130

    NIBR2130

    NIBR2130

  • Eugeroic
  • Drug for wakefulness and alertness

    of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)

    Eugeroic

    Eugeroic

    Eugeroic

  • ML337
  • Pharmaceutical compound

    for the glutamate receptor mGluR3. It has only moderate potency with an IC50 of 450 nM, but is highly selective over the closely related subtype mGluR2

    ML337

    ML337

    ML337

  • Threohydrobupropion
  • Metabolite of bupropion

    been reported to inhibit α3β4 nicotinic acetylcholine receptors, with an IC50 value of 14 μM. Threohydrobupropion circulates at higher concentrations than

    Threohydrobupropion

    Threohydrobupropion

    Threohydrobupropion

  • Nivegacetor
  • Investigational gamma-secretase modulator

    species such as Aβ38 and Aβ37. The compound demonstrates high potency with an IC50 below 10 nM for gamma-secretase modulation of APP cleavage, and importantly

    Nivegacetor

    Nivegacetor

    Nivegacetor

  • Gallinamide A
  • Chemical compound

    a IC50 5.0 ug/mL, nonetheless, human cathepsin L is involved in many diseases, gallinamide A was tested in HeLa cervical cancer cells with a IC50 12

    Gallinamide A

    Gallinamide A

    Gallinamide_A

  • Vabicaserin
  • Chemical compound

    5-HT)) and 5-HT2B receptor antagonist (IC50 = 29 nM). It is also a very weak antagonist at the 5-HT2A receptor (IC50 = 1,650 nM), though this action is not

    Vabicaserin

    Vabicaserin

    Vabicaserin

  • Cannabipiperidiethanone
  • Chemical compound

    affinity was measured at the CB1 and CB2 receptors and it was found to have an IC50 of 591 nM at CB1 and 968 nM at CB2, making it 2.3 times and 9.4 times weaker

    Cannabipiperidiethanone

    Cannabipiperidiethanone

    Cannabipiperidiethanone

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