Evidence map›Paper›PMID 27994749›Full record

ArticleACS medicinal chemistry letters2016

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.

William McCoull, Edward J Hennessy, Kevin Blades, Claudio Chuaqui, James E Dowling, Andrew D Ferguson, Frederick W Goldberg, Nicholas Howe, Christopher R Jones, Paul D Kemmitt and 4 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
–field-weighted citation impact
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

12 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Article
  11. Review
  12. Targeting PAK1.Biochemical Society transactions · 2017
    Review
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

14 authors.

William McCoullAstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
Edward J HennessyAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
Kevin BladesAstraZeneca , Alderley Park, Macclesfield, Cheshire, SK10 4TG, U.K.
Claudio ChuaquiAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
James E DowlingAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
Andrew D FergusonAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
Frederick W GoldbergAstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
Nicholas HoweAstraZeneca , Alderley Park, Macclesfield, Cheshire, SK10 4TG, U.K.
Christopher R JonesAstraZeneca , Alderley Park, Macclesfield, Cheshire, SK10 4TG, U.K.
Paul D KemmittAstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
Gillian LamontAstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
Jeffrey G VarnesAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
Richard A WardAstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
Bin YangAstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A bis-anilino pyrimidine PAK1 inhibitor was identified and optimized through structure-based drug design to improve PAK1 potency and achieve high kinase selectivity, giving

Indexed as

bis-anilino pyrimidinekinase selectivityLLEPAKprobe

Identifiers

PMID27994749
PMCPMC5150691

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.