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In biochemistry, the preference of ligands to bind with one receptor over another
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how
Binding_selectivity
Substance that forms a complex with a biomolecule
advantages compared to their monovalent counterparts (such as tissue selectivity, increased binding affinity, and increased potency or efficacy), bivalents may
Ligand_(biochemistry)
Topics referred to by the same term
Look up selectivity in Wiktionary, the free dictionary. Selectivity may refer to: Choice, making a selection among options Discrimination, the ability
Selectivity
Former Chinese custom
Foot binding (simplified Chinese: 缠足; traditional Chinese: 纏足; pinyin: chánzú), or footbinding, was the Chinese custom of breaking and tightly binding the
Foot_binding
Biochemical analysis procedure
estimate a specified model for the binding. Competition binding is used to determine the presence of selectivity for a particular ligand for receptor
Ligand_binding_assay
Pharmacologic characteristic
selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for
Functional_selectivity
Topics referred to by the same term
constant Binding domain Binding protein Binding selectivity Binding site BindingDB, an online database of measured binding affinities Binding potential
Binding
Computational tools
two goals: efficiency and selectivity. Efficiency involves taking into account such factors as GC-content, efficiency of binding, complementarity, secondary
In_silico_PCR
Ion channel that selectively passes K+
remove the hydration shell from the ion when it enters the selectivity filter. The selectivity filter is formed by a five residue sequence, TVGYG, termed
Potassium_channel
Beta-1 selective adrenenergic blocker medication used to treat cardiovascular diseases
degree of β1-selectivity compared to atenolol, metoprolol and betaxolol. With a selectivity ranging from being 11 to 15 times more selective for β1 over
Bisoprolol
Drugs acting on the estrogen receptor
the binding cavity of ERβ is slightly narrower than that of ERα, however, this by itself leads to modest selectivity. To attain strong selectivity, the
Selective estrogen receptor modulator
Selective_estrogen_receptor_modulator
Selective relaxant binding agents (SRBAs) are a new class of drugs that selectively encapsulates and binds neuromuscular blocking agents (NMBAs). The
Selective relaxant binding agents
Selective_relaxant_binding_agents
Chemical compound
displays fairly good selectivity, with a binding affinity for CB1 around 70x stronger than for CB2, but both its potency and selectivity are modest compared
LY-320,135
Monoclonal antibody
IgG2 monoclonal antibody that inhibits interleukin-31 signaling by binding selectively to interleukin-31 receptor alpha. It is an interleukin-31 receptor
Nemolizumab
Chemical similar in structure to vitamin B12
behavior of Sinorhizobium meliloti largely correlates with the cofactor binding selectivity of its methylmalonyl-CoA mutase (MCM). Among adenyl-cobamides, paseudovitamin
Pseudovitamin_B12
Class of drugs
conditions. Selectivity, or “binding selectivity”, describes how a ligand may bind more preferentially to one receptor than another. Selectivity can also
Adrenergic_neuron_blockers
Opioid analgesic of benzenoid class
such as desvenlafaxine and duloxetine. Tapentadol exhibits high binding selectivity and affinity for MOR, which is the principal target of the endogenous
Tapentadol
Chaperone protein
and subtype selectivity Agents exist that have high σ1 affinity but either lack subtype selectivity or have high affinity at other binding sites, thus
Sigma-1_receptor
exhibits selectivity and high affinity for NET, and are therefore generally SNRIs, compounds having substituent in the 4'-position exhibits selectivity and
Development and discovery of SSRI drugs
Development_and_discovery_of_SSRI_drugs
Chemical compound
5 μM, respectively. As such, its binding selectivity for the ERβ over the ERα was 7-fold and its functional selectivity for the ERβ over the ERα was between
DCW234
Class of drug
Manning et al. presented two high-affinity MAT-ligands with good binding selectivity for SERT and DAT, namely the 4-indolyl and 1-naphthyl arylalkylamines
Serotonin–dopamine reuptake inhibitor
Serotonin–dopamine_reuptake_inhibitor
Subdiscipline of chemistry concerned with chemical equilibrium
objective of these studies is often to find systems with a high binding selectivity of a host (receptor) for a particular target molecule or ion, the
Equilibrium_chemistry
Protein
that occurs after transcription of mRNA, regulates neuroligins' binding selectivity for α- or β-neurexins as well as the function of synapses. Alternative
Neuroligin
Scorpion toxin
effectiveness due to its selectivity. Further studies demonstrated that LqhαIT contains an NC-domain epitope, including residues critical for binding to the glycan
LqhαIT
Set of laboratory techniques for separation of mixtures
hospitals. Affinity chromatography Aqueous normal-phase chromatography Binding selectivity Chiral analysis Chromatofocusing Chromatography in blood processing
Chromatography
Unanswered question in the study of consciousness
(cognitive) binding problem is the problem of how objects, background, and abstract or emotional features are combined into a single experience. The binding problem
Binding_problem
Pharmaceutical compound
most tryptamines are highly non-selective in terms of binding to serotonin receptors, 1-propyl-5-MeO-AMT shows selectivity for the serotonin 5-HT2A receptor
1-Propyl-5-MeO-AMT
Chemical compound
Both compounds showed moderate binding selectivity against the 5-HT2BR and 5-HT2CR, and overall better selectivity profiles than those of classic psychedelic
(R)-70
Prokaryotic potassium ion channel
channels was centered on the use of small toxin binding to reveal the location of the pore and selectivity filter among channel residues. MacKinnon's group
KcsA_potassium_channel
Invention of new medications based on knowledge of a biological target
class of drugs and computational methods for improving the affinity, selectivity, and stability of these protein-based therapeutics have also been developed
Drug_design
Psychedelic drug
5-HT2A receptor, 100-fold selectivity for the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor, and 46-fold selectivity for the serotonin 5-HT2A
25CN-NBOH
Chemical compound
14-fold binding selectivity for the ERβ over the ERα (Ki = 0.19 nM versus 2.68 nM, respectively). However, it shows 32-fold functional selectivity for activation
Erteberel
Pharmaceutical compound
Cys-797 residue of the ATP-binding site of EGFR via a Michael addition to form a covalent bond. It has binding selectivity for T790M mutant over wild‑type
Firmonertinib
Electrostatic phenomenon
strong affinity to the binding site. This conductivity-selectivity paradox has been explained as being a consequence of selective barrier-less conduction
Ionic_Coulomb_blockade
German-Swiss biochemist and protein engineer
evolution of a G protein-coupled receptor for expression, stability, and binding selectivity". Proc. Natl. Acad. Sci. U.S.A. 105 (39): 14808–14813. doi:10.1073/pnas
Andreas_Plückthun
Chemical which binds to and activates a biochemical receptor
Terms that describe this phenomenon are "functional selectivity", "protean agonism", or selective receptor modulators. As mentioned above, agonists have
Agonist
Human glycoprotein that binds to androgens and estrogens
Sex hormone-binding globulin (SHBG) or sex steroid-binding globulin (SSBG) is a glycoprotein that binds to androgens and estrogens. When produced by the
Sex_hormone–binding_globulin
Drug class
determine the selectivity. Compounds with substituents in position 2' have selectivity for NET. Compounds with substituents in position 4' are selective serotonin
Selective norepinephrine reuptake inhibitor
Selective_norepinephrine_reuptake_inhibitor
Drug discovery
caused a loss of selectivity but not loss of the β-blockade itself. This illustrated the significance of para-substitution for β1 selectivity of β-blockers
Discovery and development of beta-blockers
Discovery_and_development_of_beta-blockers
Enclosing or separating membrane in organisms acting as selective semi-permeable barrier
A biological membrane or biomembrane is a selectively permeable membrane that separates the interior of a cell from the external environment or creates
Biological_membrane
Chemical compound
lower affinity at 5-HT2B. It has similar binding affinity to 5-HT2A and 5-HT2C but shows functional selectivity for 5-HT2C. Lorcaserin PHA-57378 SCHEMBL5334361
WAY-470
Chemical compound
for the nonyloxy derivative, having a 5-HT1B binding affinity of 1.0 nM, and around 300-fold selectivity over the related 5-HT1A receptor. 5-Allyloxy-AMT
5-(Nonyloxy)tryptamine
Pharmaceutical compound
only a 3-fold binding selectivity for ERβ over the estrogen receptor alpha (ERα), it shows more than a 100-fold functional selectivity for ERβ over ERα
OSU-ERβ-12
Chemical compound
and 3.61 nM, respectively, demonstrating 9-fold binding selectivity and 11-fold functional selectivity for the ERβ over the ERα. An enantiomer of SERBA-2
SERBA-2
Mammalian protein found in humans
are crucial for ligand binding and specificity. The CALCRL/RAMP complex presents a unique ligand-binding pocket, enabling selective recognition of peptide
CALCRL
Chemical compound
for the ERβ was found to be 9 nM and it showed 62- and 160-fold binding selectivity for this receptor over the ARTooltip androgen receptor and the ERα
3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
Class of chemical compounds
loss in the treatment of obesity. Compounds are known with a pronounced selectivity for each MAT – dopamine, noradrenaline and the serotonin transporter
Phenyltropane
Chemical compound
RTI-31 is a relatively balanced reuptake inhibitor wrt the D/N/S ratio. The binding ligand affinities for the different transporters is skewed somewhat in
RTI-31
Half maximal inhibitory concentration
vivo. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. pIC 50
IC50
Ability of a substance to resist changes in structure under high temperatures
evolution of a G protein-coupled receptor for expression, stability, and binding selectivity". Proceedings of the National Academy of Sciences of the United States
Thermostability
Class of pharmacological agents
that affect the selectivity of the agonist. Visual inspection of selective β3-AR agonists revealed that they bind deep in the binding pocket of the receptors
Beta3-adrenergic_agonist
Class of proteins
Penicillin-binding proteins (PBP) are a group of proteins that are characterized by their affinity for and binding of penicillin. They are a normal constituent
Penicillin-binding_proteins
3D printing technique
in space defined by a 3D model, binding the material together to create a solid structure. It is similar to selective laser melting; the two are instantiations
Selective_laser_sintering
Canadian geneticist
2014.05.004. PMC 4048464. PMID 24856970. Klose, Rob (2005). "DNA binding selectivity of MeCP2 due to a requirement for A/T sequences adjacent to methyl-CpG"
Rob_Klose
Opioid analgesic
of (+)-cis-3-methylfentanyl with a 27,000-fold binding selectivity for mu versus delta opioid binding sites". Life Sciences. 48 (23): PL111–PL116. doi:10
Ohmefentanyl
Drug affecting hormone receptors
relatively high binding affinity for glucocorticoid receptor compared to the progesterone receptor has sparked the demand for more selective progesterone
Selective progesterone receptor modulator
Selective_progesterone_receptor_modulator
Russian dog breed
A 2020 study identified an association between GDV in Borzois and RNA Binding Motif Protein 26 (RBM26), although of unknown significance. Russian: борзо́й
Borzoi
Protein-coding gene in the species Homo sapiens
(TIP39) selectivity for the parathyroid hormone-2 (PTH2) receptor. N-terminal truncation of TIP39 reverses PTH2 receptor/PTH1 receptor binding selectivity".
Parathyroid_hormone_2
Pharmaceutical compound
reported to be subtype-selective for 5-HT2AR, which are summarized in Table 3. [...] DOHx and DOBz also have high binding selectivity for 5-HT2AR against
2,5-Dimethoxy-4-hexylamphetamine
2,5-Dimethoxy-4-hexylamphetamine
Extremely small sensors
to their sensitivity, as well as their tunability and resulting binding selectivity, nanosensors are very effective and can be designed for a wide variety
Nanosensor
Protein molecule receiving signals for a cell
currents of different ions. This is accomplished with selectivity filters, such as the selectivity filter of the K+ ion channel Guyton, Arthur C.; Hall
Receptor_(biochemistry)
Chemical compound
selectivity over 5-HT2B and 49-fold selectivity over 5-HT2C. It has a 5-HT2A Ki of 680 nM and an EC50 of 41 nM. (R)-69 is a biased agonist selective for
(R)-69
Class of drug
[non-primary source needed] although not grouped as such.[citation needed] The binding profiles of SARIs and some metabolites in terms of their affinities (Ki
Serotonin antagonist and reuptake inhibitor
Serotonin_antagonist_and_reuptake_inhibitor
Pharmaceutical compound
is only 23-fold selective for 5-HT2A receptors (Ki = 2.2 nM) relative to 5-HT2C sites (Ki = 49.8 nM) [38]. Although the selectivity of 25CN-NBOH may
2,5-Dimethoxy-4-cyanoamphetamine
2,5-Dimethoxy-4-cyanoamphetamine
Integral of drug concentration in blood plasma over time
action Mode of action Binding Receptor (biochemistry) Desensitization (medicine) Other effects of ligand Selectivity (Binding, Functional) Pleiotropy
Area under the curve (pharmacokinetics)
Area_under_the_curve_(pharmacokinetics)
Kappa opioid receptor radioligand
substantial selectivity over μ-opioid receptors (Ki = 16 ± 5 nmol/L) and δ-opioid receptors (Ki = 536 ± 234 nmol/L). It is approximately 800-fold selective for
GR-103545
Family of transport proteins
lacks the selectivity filter found in animal CNG channels as well as lacks a glycine-tyrosine-glycine-aspartate (GYGD) motif in the K+-selectivity filter
Cyclic nucleotide–gated ion channel
Cyclic_nucleotide–gated_ion_channel
American cell physiologist and biologist
2025 A role for pH dynamics regulating transcription factor DNA-binding selectivity. Nucleic Acids Res. 53(10):gkaf474. PMID: 40464693 From 1995 to 2000
Diane_Barber
Protein-coding gene in humans
6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol: antagonist, moderate binding selectivity over D1 SCH 23390 D5 receptor has been shown to form heteromers with
Dopamine_receptor_D5
Country in East Asia
Leninist principle of democratic centralism mandates that party decisions are binding on all members. China is constitutionally a unitary state divided into
China
Parasympathetic nervous system inhibitors
These agents inhibit the parasympathetic nervous system by selectively blocking the binding of ACh to its receptor in nerve cells. The nerve fibers of
Anticholinergic
Antihypertensive drug
taken orally and has minimal effects on cardiac function due to its selectivity for α1-adrenergic receptors. It lowers blood pressure by relaxing and
Prazosin
Medication for psoriasis
offers the convenience of oral administration while maintaining selective receptor binding. In phase III trials for plaque psoriasis, the most common adverse
Icotrokinra
Class of transport proteins
Altering a serine residue at the selectivity filter, labeled Sercen, to a different amino acid alters the selectivity. Gating occurs through two mechanisms:
Chloride_channel
Type of cis-regulatory element
I.; Wanke D; Birkenbihl RP; Somssich IE. (2008). "Studies on DNA-binding selectivity of WRKY transcription factors lend structural clues into WRKY-domain
W-box
Fungal metabolite
interactions with PKA in particular are used to illuminate the roles of selectivity and protein flexibility in the inhibition of kinases. For instance, the
Balanol
Codon that marks the end of a protein-coding sequence
become a protein; stop codons signal the termination of this process by binding release factors, which cause the ribosomal subunits to disassociate, releasing
Stop_codon
Mammalian protein found in Homo sapiens
EGIS-7625 – high selectivity over 5-HT2A EXT5 – highly selective EXT9 – somewhat selective LY-23,728 LY-266,097 – pKi = 9.7, 100-fold selectivity over 5-HT2A
5-HT2B_receptor
Beta blocker drug
"Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents". Japanese
Propranolol
Theoretical drug measure in pharmacology
solubility (non-polarity), low rates of ionization, or low plasma protein binding capabilities. Disease states which increase V D {\displaystyle V_{D}} include
Volume_of_distribution
Protein found in humans
Transcortin, also known as corticosteroid-binding globulin (CBG) or serpin A6, is a protein produced in the liver in animals. In humans it is encoded
Transcortin
Protein
This selectivity increases the separation between the desired antiinflammatory effects and undesired metabolic side effects of these selective glucocorticoids
Nuclear_receptor
Common application of immunostaining
involves the process of selectively identifying antigens in cells and tissue, by exploiting the principle of antibodies binding specifically to antigens
Immunohistochemistry
Pharmaceutical compound
rigorously assessed the selectivity of these earlier compounds via employment of multiple selectivity assays. TGF-8027 was less selective for the mouse serotonin
TGF-8027
Rare neurodegenerative disease
the binding affinity of the low-complexity domain, causing their respective proteins to aggregate in the cytoplasm. Once these mutant RNA-binding proteins
ALS
Purification technique for biomolecules
acid binding interactions are frequently exploited for isolation of various biomolecules. Affinity chromatography is useful for its high selectivity and
Affinity_chromatography
Public collegiate university in England
in response to threats to the climate and biodiversity. The vote is non-binding since the university controls the catering service. The vote was supported
University_of_Cambridge
Drug discovery
RN: This group determines α- or β-receptor selectivity. The larger the substituent, the greater the selectivity for the β-receptor. If t-butyl is positioned
Discovery and development of beta2 agonists
Discovery_and_development_of_beta2_agonists
Diabetes medication
only) Pharmacokinetic data Bioavailability 78% (after 10 mg dose) Protein binding ~91% Metabolism UGT1A9 (major), CYP (minor) Metabolites Dapagliflozin 3-O-glucuronide
Dapagliflozin
Antihistamine medication
(Ki ≈ 6 nM) and shows about 600-fold selectivity for H1 over a panel of other receptors and ion channels. Binding is stereoselective: the (R)-enantiomer
Levocetirizine
Class of antidepressant medication
for inhibition of serotonin reuptake over norepinephrine reuptake. The selectivity ratios are approximately 1:30 for venlafaxine, 1:10 for duloxetine, and
Selective serotonin reuptake inhibitor
Selective_serotonin_reuptake_inhibitor
Class of cell surface receptors
based on phenylaminotetralin (PAT) ligands, but later work showed this binding corresponded to the histamine H1 receptor; "sigma-3" is not recognized
Sigma_receptor
Country in Central Europe (1949–1990)
the subsequent Unification Treaty of 31 August 1990 – that is, through a binding agreement between the former Democratic Republic and the Federal Republic
East_Germany
ligand with high affinity and selectivity for the (+)-MK801-insensitive [3H]1-]1-(2-thienyl)cyclohexyl]piperidine binding site (PCP site 2) of guinea pig
PCP_site_2
Chemical compound
and is one the most selective agonists reported to date, with high binding affinity to 5-HT2AR (Ki = 2.5 nM) and 124-fold selectivity towards the 5-HT2CR
DMBMPP
Protein that regulates the rate of DNA transcription
sequence-specific DNA-binding factor) is a protein that controls the rate of transcription of genetic information from DNA to messenger RNA, by binding to DNA sequences
Transcription_factor
Regulation of enzyme activity
by the binding of a ligand at an allosteric site topographically distinct from the orthosteric site. Due to the often high receptor selectivity and lower
Allosteric_regulation
G-protein-coupled receptor
each case, agonist binding results in an increase in intracellular calcium levels. However, orexin-B shows a 5- to 10-fold selectivity for orexin receptor
Orexin_receptor
Gene family
The ABC transporters, also known as ATP-binding cassette transporters, are a transport system superfamily that is one of the largest and possibly one
ABC_transporter
Amino acid peptide
alpha-helical secondary structures, which support biological activity and binding selectivity. Multiple urocortin genes are present in vertebrate lineages as a
Urocortin_III
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BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
BINDING SELECTIVITY
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