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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
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
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
constant Binding domain Binding protein Binding selectivity Binding site BindingDB, an online database of measured binding affinities Binding potential
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
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
Pharmacologic characteristic
selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for
Functional_selectivity
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
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
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
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
make the resultant derivative display much greater efficacy, affinity, selectivity &/or strength than even the parent compound; which otherwise was compromised
List_of_cocaine_analogues
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
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
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
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
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
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
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
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
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
Direct vote on a specific proposal
representatives) on a proposal, law, or political issue. A referendum may be either binding, resulting in the adoption of a new policy, or consultive (or advisory)
Referendum
Protein-coding gene in humans
first demonstration of functional selectivity with dopamine receptors. Dinapsoline – full agonist with 5-fold selectivity for D1-like receptors over D2 Dinoxyline –
Dopamine_receptor_D1
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
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 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
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
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
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
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
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
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
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
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
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
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
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
Protein found in humans
chitinase-like protein (SI-CLP) reveals a saccharide-binding cleft with lower sugar-binding selectivity". The Journal of Biological Chemistry. 285 (51): 39898–904
Chitinase domain-containing protein 1
Chitinase_domain-containing_protein_1
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
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
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
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
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
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
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
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
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 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
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
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
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
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
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
Chemical compound
nonbenzodiazepine anxiolytic. It is a subtype-selective partial agonist at GABAA receptors, binding selectively to GABAA receptor complexes bearing α2 and
TP-13
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)
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
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
Agent in biochemistry
(2018-08-06). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". International Journal of Neuropsychopharmacology. 21 (10): 962–977
Inverse_agonist
Protein-coding gene in the species Homo sapiens
1016/0022-2836(92)90984-R. PMID 1311770. Kirsch T, Pfäffle M (Sep 1992). "Selective binding of anchorin CII (annexin V) to type II and X collagen and to chondrocalcin
Annexin_A5
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
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
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)
Chemical compound
bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved
Enzastaurin
Chemical compound
stroke that had been conducted. Gavestinel is an NMDA antagonist, binding selectively to the glycine site on the NMDA receptor complex, rather than the
Gavestinel
Small molecule (PROTAC)
proteasome. Because PROTACs need only to bind their targets with high selectivity (rather than inhibit the target protein's enzymatic activity), efforts
Proteolysis_targeting_chimera
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
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 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
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
potent and selective ligand for the sigma-1 receptor, with a reported binding affinity of Ki = 0.08 ± 0.01 nM, and 17,212 times selectivity over the sigma-2
PD_144418
Enzyme involved in blood coagulation in humans
activated Factor X (Xa). The activity of factor Xa is greatly enhanced by binding to activated Factor V (Va), termed the prothrombinase complex. Prothrombin
Thrombin
Protein-coding gene in the species Homo sapiens, named for ketazocine
(PET) imaging studies with the KOR-selective radioligand [11C]GR-103545 in non-human primates showed high binding potential (BPND > 1.3) in the pituitary
Κ-opioid_receptor
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
Chemical compound
noradrenaline. With a binding affinity (Ki) of 55 nM at DAT and 28.4 nM at SERT but only 4030 nM at NET, RTI-83 has reasonable selectivity for DAT/SERT over
RTI-83
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
Class of enzymes
in the lower binding pocket may lie too far away for interaction with the inhibitor and therefore might be irrelevant for EHNA selectivity. However the
Phosphodiesterase_2
Type of catalysis involving reactants & catalysts in different phases of matter
a set of binding energies that can change the selectivity toward a specific product "scale" with each other, thus to improve the selectivity one has to
Heterogeneous_catalysis
Protein-coding gene in the species Homo sapiens
the type I PACAP receptor: isolation, characterization and ligand binding/selectivity determinants". Journal of Neuroendocrinology. 11 (12): 941–9. doi:10
ADCYAP1R1
Chemical compound
receptor binding studies.89 However, it is now known that 18 also behaves as a partial agonist at human 5-HT2C receptors with low binding selectivity relative
ORG-12962
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
Protein helix–loop–helix motif
This high selectivity is due to the relatively rigid coordination geometry, the presence of multiple charged amino acid side chains in the binding site, as
EF_hand
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
Antihypertensive drug
minimal effect on cardiac function due to its α1-adrenergic receptor selectivity. When prazosin is started, however, heart rate and contractility can
Prazosin
Chemical compound
but with different binding affinity for the δ1 and δ2 subtypes, which makes it useful for distinguishing the subtype selectivity of drugs acting at the
Naltriben
Type of chemical used to kill unwanted plants
safeners enhance the selectivity by boosting herbicide resistance by the crop but allowing the herbicide to damage the weed. Selectivity is determined by
Herbicide
Medication
of an improved selectivity profile, with selectivity of S1P1 over S1P5 receptors at 27‐fold, and selectivity for S1P1 over S1P2, S1P3, and S1P4 receptors
Ozanimod
Chemical compound
agonist at the 5-HT1A and 5-HT1D serotonin receptors, with around 3x selectivity for 5-HT1D. 5-Benzyloxytryptamine 5-Carboxamidotryptamine 5-Ethoxy-DMT
5-Ethyl-DMT
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".
TIP39
Chemical compound
Merck, Sharp and Dohme, which acts as a subtype-selective inverse agonist at the benzodiazepine binding site on the GABAA receptor. It binds to α1, α2
Α5IA
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
Selective relaxant binding agent
rocuronium and vecuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). It is marketed by Merck. The most common side effects
Sugammadex
Mammalian protein found in humans
specificity, and cGMP-binding to the allosteric sites stimulates binding of PDE5 inhibitors at the catalytic site. The kinetics of inhibitor binding and inhibition
CGMP-specific phosphodiesterase type 5
CGMP-specific_phosphodiesterase_type_5
Enzyme
been developed that showed high selectivity for MMP-11. Derivatives based on phenyl rings showed the best selectivity. MMP-11 could be a useful target
Metalloprotease_inhibitor
Protein-coding gene in the species Homo sapiens
polycomb group protein PCGF1 in complex with BCOR reveals basis for binding selectivity of PCGF homologs". Structure. 21 (4): 665–71. doi:10.1016/j.str.2013
PCGF1
Branch of pharmacology
term structural or functional changes Disturbed homeostasis Functional selectivity (biased Agonism) - preferentially activate certain pathways over others
Pharmacodynamics
Chemical compound
2009). "On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine". Chemical Biology & Drug
Staurosporine
Main receptor for most antipsychotic drugs
are, in general, very unselective, at best selective only for the "D2-like family" receptors and so binding to D2, D3 and D4, and often also to many other
Dopamine_receptor_D2
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
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