Evidence map›Paper›PMID 42157838›Full record

ArticleACS medicinal chemistry letters2026

Discovery of BMS-159, an Orally Active Imidazotriazine Pan-CK2 Inhibitor for the Treatment of Cancer.

Christine M Tarby, Amy Hart, Honghe Wan, Liqi He, John Tokarski, Brian Fink, Yufen Zhao, Tram Huynh, Ashvinikumar Gavai, Kurt Zimmermann and 25 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

35 authors.

Christine M TarbyBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Amy HartBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.ORCID https://orcid.org/0000-0002-3739-319X
Honghe WanBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Liqi HeBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
John TokarskiBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Brian FinkBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Yufen ZhaoBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Tram HuynhBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Ashvinikumar GavaiBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.ORCID https://orcid.org/0000-0002-6067-4176
Kurt ZimmermannBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Gregory ViteBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Dolatrai VyasBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Jennifer InghrimBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Mary ObermeierBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Aberra FuraBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Paul ElzingaBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
John HuntBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Urvashi RoongtaBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Benjamin HenleyBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Jonathan LippyBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Arvind MathurBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.ORCID https://orcid.org/0000-0003-3146-8485
Dauh Rurng WuBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Peng LiBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Nirmala RaghavanBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Gerry EverlofBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Brent RupnowBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Francis LeeBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Joseph FargnoliBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Jeffrey TredupBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Susan E KieferBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Deepa CalamburBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
Anuradha GuptaBiocon-Bristol Myers Squibb R&D Centre, Syngene, Biocon Park, Bommasandra Phase IV, Jigani Road, Bangalore-560099, India.ORCID https://orcid.org/0000-0002-4211-1441
Muthalagu VetrichelvanBiocon-Bristol Myers Squibb R&D Centre, Syngene, Biocon Park, Bommasandra Phase IV, Jigani Road, Bangalore-560099, India.ORCID https://orcid.org/0000-0001-7201-4143
Murugaiah A M SubbaiahBiocon-Bristol Myers Squibb R&D Centre, Syngene, Biocon Park, Bommasandra Phase IV, Jigani Road, Bangalore-560099, India.ORCID https://orcid.org/0000-0001-5707-966X
Ashok V PurandareBristol-Myers Squibb R&D, U.S. Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Casein kinase 2 (CK2), comprising the catalytic subunits CK2α and CK2α', is a highly conserved and constitutively active serine/threonine kinase that is implicated in oncogenic signaling and tumor maintenance, making it an attractive therapeutic target. We report a medicinal chemistry campaign that delivered an imidazotriazine pan-CK2 series culminating in BMS-135 and its phosphate prodrug BMS-159. Structure-guided design enabled a scaffold hop from imidazopyridazine to imidazotriazine that improved kinome selectivity while preserving critical hinge and Lys68 interactions. Iterative SAR optimization mitigated hERG liability by modulating distal basicity and enhanced metabolic stability via a C8

Indexed as

AnticancerBMS-135BMS-159Casein kinase 2ImidazotriazineProdrugScaffold hopping

Identifiers

PMID42157838
PMCPMC13181496

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.