Matches in DBpedia 2016-04 for { <http://dbpedia.org/resource/Hit_to_lead> ?p ?o }
Showing triples 1 to 78 of
78
with 100 triples per page.
- Hit_to_lead abstract "Hit to lead (H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds. These lead compounds undergo more extensive optimization in a subsequent step of drug discovery called lead optimization (LO). The drug discovery process generally follows the following path that includes a hit to lead stage: target validation (TV) → assay development → high-throughput screening → hit to lead (H2L) → lead optimization (LO) → preclinical drug development → clinical drug developmentThe hit to lead stage starts with confirmation and evaluation of the initial screening hits and is followed by synthesis of analogs (hit expansion). Typically the initial screening hits display binding affinities for their biological target in the micromolar (10−6 molar concentration) range. Through limited H2L optimization, the affinities of the hits are often improved by several orders of magnitude to the nanomolar (10−9 M) range. The hits also undergo limited optimization to improve metabolic half life so that the compounds can be tested in animal models of disease and also to improve selectivity against other biological targets binding that may result in undesirable side effects.On average, only one in every 5,000 compounds that enters drug discovery to the stage of pre-clinical development becomes an approved drug.".
- Hit_to_lead wikiPageID "7474102".
- Hit_to_lead wikiPageLength "9310".
- Hit_to_lead wikiPageOutDegree "60".
- Hit_to_lead wikiPageRevisionID "690414976".
- Hit_to_lead wikiPageWikiLink Binding_selectivity.
- Hit_to_lead wikiPageWikiLink Biological_half-life.
- Hit_to_lead wikiPageWikiLink Biological_target.
- Hit_to_lead wikiPageWikiLink Category:Drug_discovery.
- Hit_to_lead wikiPageWikiLink Category:Pharmaceutical_industry.
- Hit_to_lead wikiPageWikiLink Cheminformatics.
- Hit_to_lead wikiPageWikiLink Combinatorial_chemistry.
- Hit_to_lead wikiPageWikiLink Conformational_change.
- Hit_to_lead wikiPageWikiLink Cytochrome_P450.
- Hit_to_lead wikiPageWikiLink Cytotoxicity.
- Hit_to_lead wikiPageWikiLink Drug_design.
- Hit_to_lead wikiPageWikiLink Drug_development.
- Hit_to_lead wikiPageWikiLink Drug_discovery.
- Hit_to_lead wikiPageWikiLink Drug_metabolism.
- Hit_to_lead wikiPageWikiLink Druglikeness.
- Hit_to_lead wikiPageWikiLink Dual-polarization_interferometry.
- Hit_to_lead wikiPageWikiLink Dynamic_light_scattering.
- Hit_to_lead wikiPageWikiLink EC50.
- Hit_to_lead wikiPageWikiLink Fragment-based_lead_discovery.
- Hit_to_lead wikiPageWikiLink High-content_screening.
- Hit_to_lead wikiPageWikiLink High-throughput_screening.
- Hit_to_lead wikiPageWikiLink IC50.
- Hit_to_lead wikiPageWikiLink Intrinsic_activity.
- Hit_to_lead wikiPageWikiLink Isothermal_titration_calorimetry.
- Hit_to_lead wikiPageWikiLink Lead_compound.
- Hit_to_lead wikiPageWikiLink Ligand_(biochemistry).
- Hit_to_lead wikiPageWikiLink Ligand_efficiency.
- Hit_to_lead wikiPageWikiLink Lipophilic_efficiency.
- Hit_to_lead wikiPageWikiLink Lipophilicity.
- Hit_to_lead wikiPageWikiLink Microscale_thermophoresis.
- Hit_to_lead wikiPageWikiLink Model_organism.
- Hit_to_lead wikiPageWikiLink Molar_concentration.
- Hit_to_lead wikiPageWikiLink Nuclear_magnetic_resonance.
- Hit_to_lead wikiPageWikiLink Organic_chemistry.
- Hit_to_lead wikiPageWikiLink P-glycoprotein.
- Hit_to_lead wikiPageWikiLink Partition_coefficient.
- Hit_to_lead wikiPageWikiLink Patent_infringement.
- Hit_to_lead wikiPageWikiLink Pharmaceutical_industry.
- Hit_to_lead wikiPageWikiLink Pharmacokinetics.
- Hit_to_lead wikiPageWikiLink Pre-clinical_development.
- Hit_to_lead wikiPageWikiLink Quantitative_structure–activity_relationship.
- Hit_to_lead wikiPageWikiLink Receptor–ligand_kinetics.
- Hit_to_lead wikiPageWikiLink Serum_albumin.
- Hit_to_lead wikiPageWikiLink Small_molecule.
- Hit_to_lead wikiPageWikiLink Stoichiometry.
- Hit_to_lead wikiPageWikiLink Structural_analog.
- Hit_to_lead wikiPageWikiLink Surface_plasmon_resonance.
- Hit_to_lead wikiPageWikiLink Thermodynamics.
- Hit_to_lead wikiPageWikiLinkText ""hits"".
- Hit_to_lead wikiPageWikiLinkText "Hit to lead".
- Hit_to_lead wikiPageWikiLinkText "hit to lead optimization".
- Hit_to_lead wikiPageWikiLinkText "hit to lead".
- Hit_to_lead wikiPageWikiLinkText "lead generation".
- Hit_to_lead wikiPageWikiLinkText "screening hits".
- Hit_to_lead wikiPageUsesTemplate Template:Columns-list.
- Hit_to_lead wikiPageUsesTemplate Template:Drug_design.
- Hit_to_lead wikiPageUsesTemplate Template:Reflist.
- Hit_to_lead subject Category:Drug_discovery.
- Hit_to_lead subject Category:Pharmaceutical_industry.
- Hit_to_lead hypernym Stage.
- Hit_to_lead type Person.
- Hit_to_lead type Industry.
- Hit_to_lead type Pharmaceutic.
- Hit_to_lead type Redirect.
- Hit_to_lead type Science.
- Hit_to_lead comment "Hit to lead (H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds. These lead compounds undergo more extensive optimization in a subsequent step of drug discovery called lead optimization (LO).".
- Hit_to_lead label "Hit to lead".
- Hit_to_lead sameAs Q13611503.
- Hit_to_lead sameAs ממולקולת_מטרה_למולקולה_מובילה.
- Hit_to_lead sameAs m.0262vq3.
- Hit_to_lead sameAs Q13611503.
- Hit_to_lead wasDerivedFrom Hit_to_lead?oldid=690414976.
- Hit_to_lead isPrimaryTopicOf Hit_to_lead.