Evidence map›Paper›PMID 31749904›Full record

ArticleACS medicinal chemistry letters2019

Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.

Curt D Haffner, Adam K Charnley, Christopher J Aquino, Linda Casillas, Máire A Convery, Julie A Cox, Mark A Elban, Nicole C Goodwin, Peter J Gough, Pamela A Haile and 16 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
  5. RIPK2: a promising target for cancer treatment.Frontiers in pharmacology · 2023
    Review
  6. 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

26 authors.

Curt D HaffnerGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Adam K CharnleyGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Christopher J AquinoGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Linda CasillasGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Máire A ConveryGlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, U.K.
Julie A CoxGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Mark A ElbanGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Nicole C GoodwinGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Peter J GoughGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Pamela A HaileGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Terry V HughesGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Beth Knapp-ReedGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Constantine KreatsoulasGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Ami S LakdawalaGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Huijie LiGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Yiqian LianGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
David LipshutzGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
John F MehlmannGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Michael OuelletteGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Joseph RomanoGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Lisa ShewchukGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Arthur ShuGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Bartholomew J VottaGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Huiqiang ZhouGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
John BertinGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Robert W MarquisGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Herein we report the discovery of pyrazolocarboxamides as novel, potent, and kinase selective inhibitors of receptor interacting protein 2 kinase (RIP2). Fragment based screening and design principles led to the identification of the inhibitor series, and X-ray crystallography was used to inform key structural changes. Through key substitutions about the N1 and C5 N positions on the pyrazole ring significant kinase selectivity and potency were achieved. Bridged bicyclic pyrazolocarboxamide

Identifiers

PMID31749904
PMCPMC6862347

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.