The following articles (labelled with PubMed ID or TBD) are for your reviewPMID | Article Title | Published | Deposition |
---|
36966977 |
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS. |
01-MAY-2023 |
22-APR-2024 |
30891122 |
Discovery of VU2957 (Valiglurax): An mGlu |
14-MAR-2019 |
22-APR-2024 |
36528230 |
Persistent challenges in the development of an mGlu |
15-JAN-2023 |
20-APR-2024 |
36228968 |
Discovery of a potent M |
15-DEC-2022 |
20-APR-2024 |
34917258 |
Ring Size as an Independent Variable in Cyclooligomeric Depsipeptide Antiarrhythmic Activity. |
09-DEC-2021 |
19-APR-2024 |
US11752138 |
Treating primary or idiopathic hyperoxaluria with small molecule inhibitors of lactate dehydrogenase |
12-SEP-2023 |
20-OCT-2023 |
36113671 |
Discovery of a potent M |
15-NOV-2022 |
26-JUN-2023 |
35417155 |
Development of |
28-APR-2022 |
25-JUN-2023 |
35944850 |
Development and profiling of mGlu |
15-OCT-2022 |
18-JUN-2023 |
US11596639 |
Substituted indole Mcl-1 inhibitors |
07-MAR-2023 |
23-APR-2023 |
34710625 |
Discovery of structurally distinct tricyclic M |
01-DEC-2021 |
04-MAR-2023 |
34413964 |
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M |
12-AUG-2021 |
24-AUG-2022 |
34461178 |
Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds. |
15-OCT-2021 |
24-AUG-2022 |
33771585 |
Optimization of ether and aniline based inhibitors of lactate dehydrogenase. |
01-JUN-2021 |
20-AUG-2022 |
US11319304 |
Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
03-MAY-2022 |
07-AUG-2022 |
US11242342 |
Isoquinoline amine compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
08-FEB-2022 |
10-JUN-2022 |
US11208415 |
Substituted indole Mcl-1 inhibitors |
28-DEC-2021 |
03-MAY-2022 |
33556572 |
Discovery and optimization of a novel CNS penetrant series of mGlu |
01-APR-2021 |
29-MAR-2022 |
32750526 |
Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors. |
15-SEP-2020 |
28-MAR-2022 |
32371100 |
Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu |
01-JUL-2020 |
28-MAR-2022 |
32890686 |
Synthesis and SAR of a series of mGlu |
15-NOV-2020 |
25-MAR-2022 |
33253881 |
Lead optimization of the VU0486321 series of mGlu |
15-JAN-2021 |
24-MAR-2022 |
32944146 |
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu |
10-SEP-2020 |
22-MAR-2022 |
30503632 |
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu |
15-JAN-2019 |
21-MAR-2022 |
US11149022 |
Antagonists of the muscarinic acetylcholine receptor M4 |
19-OCT-2021 |
13-MAR-2022 |
US10968227 |
Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
06-APR-2021 |
09-OCT-2021 |
US10954193 |
Substituted indole Mcl-1 inhibitors |
23-MAR-2021 |
28-SEP-2021 |
31784320 |
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M |
01-FEB-2020 |
12-AUG-2021 |
31787491 |
Discovery of structurally distinct tricyclic M |
15-FEB-2020 |
12-AUG-2021 |
32223236 |
Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. |
23-APR-2020 |
11-AUG-2021 |
US10844032 |
Substituted benzofuran, benzothiophene and indole Mcl-1 inhibitors |
24-NOV-2020 |
06-JUL-2021 |
US10844044 |
WDR5 inhibitors and modulators |
24-NOV-2020 |
06-JUL-2021 |
US10807959 |
WDR5-MLL1 inhibitors and modulators |
20-OCT-2020 |
11-JUN-2021 |
US10793514 |
Glutamine transport inhibitors and methods for treating cancer |
06-OCT-2020 |
14-MAY-2021 |
27503678 |
Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes. |
15-SEP-2016 |
28-FEB-2021 |
30728114 |
Fragment-based screening of programmed death ligand 1 (PD-L1). |
15-MAR-2019 |
27-FEB-2021 |
31724864 |
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. |
26-DEC-2019 |
26-FEB-2021 |
30910459 |
Surveying heterocycles as amide bioisosteres within a series of mGlu |
15-MAY-2019 |
24-FEB-2021 |
30580918 |
Novel M |
01-FEB-2019 |
23-FEB-2021 |
31248774 |
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M |
15-AUG-2019 |
23-FEB-2021 |
30528696 |
Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. |
15-JAN-2019 |
22-FEB-2021 |
31537424 |
Discovery of a novel 3,4-dimethylcinnoline carboxamide M |
01-NOV-2019 |
22-FEB-2021 |
31358468 |
Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu |
15-SEP-2019 |
20-FEB-2021 |
31938459 |
Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy. |
09-JAN-2020 |
19-FEB-2021 |
30247901 |
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu |
10-JAN-2019 |
18-FEB-2021 |
US10538491 |
4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators |
21-JAN-2020 |
09-NOV-2020 |
US10533010 |
Substituted indole Mcl-1 inhibitors |
14-JAN-2020 |
02-NOV-2020 |
US10501466 |
WDR5 inhibitors and modulators |
10-DEC-2019 |
12-OCT-2020 |
US10508105 |
Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
17-DEC-2019 |
12-OCT-2020 |
US10487087 |
Positive allosteric modulators of the GLP-1 receptor |
26-NOV-2019 |
20-SEP-2020 |
23687559 |
The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
09-MAY-2013 |
01-SEP-2020 |
24060487 |
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib. |
01-NOV-2013 |
01-SEP-2020 |
US10399948 |
Negative allosteric modulators of metabotropic glutamate receptor 3 |
03-SEP-2019 |
24-AUG-2020 |
29958762 |
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu |
15-AUG-2018 |
17-AUG-2020 |
29705142 |
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. |
01-JUN-2018 |
16-AUG-2020 |
29037946 |
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M |
15-NOV-2017 |
15-AUG-2020 |
29057060 |
Discovery of VU6005649, a CNS Penetrant mGlu |
12-OCT-2017 |
04-JUL-2020 |
29856609 |
Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. |
26-JUL-2018 |
24-JUN-2020 |
29259756 |
VU6010608, a Novel mGlu |
14-DEC-2017 |
23-JUN-2020 |
US10294214 |
Positive allosteric modulators of human melanocortin-4 receptor |
21-MAY-2019 |
10-MAR-2020 |
28958625 |
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. |
01-NOV-2017 |
25-JAN-2020 |
28866269 |
Discovery of a novel, CNS penetrant M |
15-SEP-2017 |
19-JAN-2020 |
US10239887 |
Positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
26-MAR-2019 |
30-DEC-2019 |
US10227343 |
Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
12-MAR-2019 |
27-DEC-2019 |
28428041 |
Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin. |
15-JUN-2017 |
30-NOV-2019 |
US10221175 |
Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1 |
05-MAR-2019 |
27-OCT-2019 |
US10221172 |
Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
05-MAR-2019 |
27-OCT-2019 |
US10189805 |
Metabolism probes for therapy and diagnosis |
29-JAN-2019 |
25-MAY-2019 |
28103022 |
Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core. |
23-FEB-2017 |
01-MAY-2019 |
US9550778 |
Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5 |
24-JAN-2017 |
18-SEP-2018 |
US9676782 |
Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of metabotropic glutamate receptor 3 |
13-JUN-2017 |
07-AUG-2018 |
27353534 |
New structure-activity relationships of N-acetamide substituted pyrazolopyrimidines as pharmacological ligands of TSPO. |
19-JUL-2016 |
06-OCT-2017 |
US9453017 |
Antiviral therapies with phospholipase D inhibitors |
27-SEP-2016 |
05-SEP-2017 |
27080176 |
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists. |
16-JUN-2016 |
14-JUL-2017 |
US9346803 |
Indomethacin analogs for the treatment of castrate-resistant prostate cancer |
24-MAY-2016 |
05-JUN-2017 |
24047900 |
Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity. |
01-NOV-2013 |
25-FEB-2017 |
US9255103 |
Substituted pyrazolo[1,5-a]pyrazines as mGluR5 receptor modulators |
09-FEB-2016 |
20-DEC-2016 |
26426481 |
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics |
22-OCT-2015 |
14-DEC-2016 |
US9192603 |
Heterocyclic sulfone mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
24-NOV-2015 |
19-SEP-2016 |
US9180192 |
mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
10-NOV-2015 |
15-AUG-2016 |
US9163015 |
Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
20-OCT-2015 |
18-JUL-2016 |
US9127005 |
Isoform selective phospholipase D inhibitors |
08-SEP-2015 |
09-MAY-2016 |
25466173 |
Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition. |
03-DEC-2014 |
17-MAR-2016 |
25221667 |
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. |
15-SEP-2014 |
08-MAR-2016 |
US9040694 |
Compounds and methods useful for directing stem cell differentiation |
26-MAY-2015 |
21-DEC-2015 |
25384256 |
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. |
20-FEB-2015 |
15-OCT-2015 |
US8796295 |
Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same |
05-AUG-2014 |
12-JAN-2015 |
24164599 |
Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). |
27-NOV-2013 |
25-JUL-2014 |
US8598345 |
Substituted heteroarylamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same |
03-DEC-2013 |
14-APR-2014 |
24482730 |
Rational Design of Novel Pyridinol-Fused Ring Acetaminophen Analogues. |
08-AUG-2013 |
13-APR-2014 |
23916258 |
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. |
23-AUG-2013 |
13-APR-2014 |
24050755 |
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254). |
24-OCT-2013 |
13-APR-2014 |
US8569308 |
Substituted heteroarylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same |
29-OCT-2013 |
24-FEB-2014 |
23519677 |
Improving the affinity of SL0101 for RSK using structure-based design. |
14-FEB-2012 |
24-SEP-2013 |
11964599 |
Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. |
19-APR-2002 |
22-MAY-2013 |
20732812 |
3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators. |
13-SEP-2010 |
22-MAY-2013 |
7861418 |
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
21-MAR-1995 |
31-OCT-2012 |
3172140 |
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors. |
18-NOV-1988 |
16-OCT-2012 |
8278895 |
Evaluation of 5-[18F]fluoropropylepidepride as a potential PET radioligand for imaging dopamine D2 receptors. |
XX-XXX-1993 |
02-JAN-2012 |
3139864 |
Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus. |
XX-XXX-1988 |
24-NOV-2011 |
18022567 |
Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. |
XX-NOV-2007 |
04-AUG-2011 |
19136975 |
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
XX-FEB-2009 |
25-FEB-2011 |
20020776 |
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. |
19-FEB-2010 |
11-FEB-2011 |
19443215 |
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. |
29-MAY-2009 |
25-AUG-2010 |
19299128 |
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity. |
03-APR-2009 |
11-JAN-2010 |
18800848 |
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential. |
27-OCT-2008 |
11-JAN-2010 |
18674906 |
A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride. |
11-AUG-2008 |
11-JAN-2010 |
8064797 |
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
22-SEP-1994 |
10-NOV-2009 |
17766114 |
Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots. |
18-SEP-2007 |
10-NOV-2009 |
16183285 |
Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots. |
19-OCT-2005 |
10-NOV-2009 |
16784853 |
High affinity inhibitors of the dopamine transporter (DAT): novel biotinylated ligands for conjugation to quantum dots. |
31-JUL-2006 |
10-NOV-2009 |
15887968 |
Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1. |
12-MAY-2005 |
10-NOV-2009 |
1694546 |
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors. |
06-AUG-1990 |
10-NOV-2009 |
1967652 |
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
09-MAR-1990 |
10-NOV-2009 |
2571728 |
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
01-NOV-1989 |
10-NOV-2009 |
19354253 |
Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase. |
14-MAY-2009 |
08-JUN-2009 |