Evidence map›Paper›PMID 29204742›Full record

ArticleThe AAPS journal2017

Target and Tissue Selectivity Prediction by Integrated Mechanistic Pharmacokinetic-Target Binding and Quantitative Structure Activity Modeling.

Anna H C Vlot, Wilhelmus E A de Witte, Meindert Danhof, Piet H van der Graaf, Gerard J P van Westen, Elizabeth C M de Lange

Open access · hybridAbstract read
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In one paragraph

Article in The AAPS journal, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.5field-weighted citation impact, top 18% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 19 citations in OpenAlex.

  1. Electrochemical modulation enhances the selectivity of peripheral neurostimulation in vivo.Proceedings of the National Academy of Sciences of the United States of America · 2022
    Article
  2. Engineering Binders with Exceptional Selectivity.Methods in molecular biology (Clifton, N.J.) · 2022
    Article
  3. Article
  4. Binding kinetics of ligands acting at GPCRs.Molecular and cellular endocrinology · 2019
    Review
  5. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 2 institutions in 2 countries.

Anna H C VlotDivision of Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands.
Wilhelmus E A de WitteDivision of Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands.
Meindert DanhofDivision of Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands.
Piet H van der GraafDivision of Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands.
Gerard J P van WestenDivision of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands.
Elizabeth C M de LangeDivision of Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333, CC, Leiden, The Netherlands. ecmdelange@lacdr.leidenuniv.nl.
Leiden University · NLCentre for Human Drug Research · NL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Selectivity is an important attribute of effective and safe drugs, and prediction of in vivo target and tissue selectivity would likely improve drug development success rates. However, a lack of understanding of the underlying (pharmacological) mechanisms and availability of directly applicable predictive methods complicates the prediction of selectivity. We explore the value of combining physiologically based pharmacokinetic (PBPK) modeling with quantitative structure-activity relationship (QSAR) modeling to predict the influence of the target dissociation constant (K

Indexed as

Models, BiologicalPharmacokineticsQuantitative Structure-Activity RelationshipHumansOrgan SpecificityReceptor, Cannabinoid, CB1Receptor, Cannabinoid, CB1kinetic selectivityphysiologically based pharmacokinetic modelingquantitative structure-activity relationshiptarget-mediated drug dispositiontissue selectivity

Identifiers

PMID29204742
OpenAlexW2773757188

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.