Evidence map›Paper›PMID 27660686›Full record

ArticleACS medicinal chemistry letters2016

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.

Heather J Finlay, James A Johnson, John L Lloyd, Ji Jiang, James Neels, Prashantha Gunaga, Abhisek Banerjee, Naveen Dhondi, Anjaneya Chimalakonda, Sandhya Mandlekar and 5 more

Abstract read
PubMed Full text at PMC Publisher
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 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

15 authors.

Heather J FinlayDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
James A JohnsonDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
John L LloydDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Ji JiangDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
James NeelsDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Prashantha GunagaDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Biocon Bristol-Myers Squibb Research Center (BBRC) , Bangalore 560099, India.
Abhisek BanerjeeDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Biocon Bristol-Myers Squibb Research Center (BBRC) , Bangalore 560099, India.
Naveen DhondiDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Biocon Bristol-Myers Squibb Research Center (BBRC) , Bangalore 560099, India.
Anjaneya ChimalakondaDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Sandhya MandlekarDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Biocon Bristol-Myers Squibb Research Center (BBRC) , Bangalore 560099, India.
Mary Lee ConderDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Harinath SaleDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Biocon Bristol-Myers Squibb Research Center (BBRC) , Bangalore 560099, India.
Dezhi XingDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Paul LevesqueDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Ruth R WexlerDepartments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A new series of phenylquinazoline inhibitors of Kv 1.5 is disclosed. The series was optimized for Kv 1.5 potency, selectivity versus hERG, pharmacokinetic exposure, and pharmacodynamic potency. 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (13k) was identified as a potent and ion channel selective inhibitor with robust efficacy in the preclinical rat ventricular effective refractory period (VERP) model and the rabbit atrial effective refractory period (AERP) model.

Indexed as

atrial effective refractory periodKv 1.5phenylquinazolineventricular effective refractory period

Identifiers

PMID27660686
PMCPMC5018869

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.