360 articles for thisTarget
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Article Title
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216
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Amgen
4
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Amgen
18
Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.
Amgen
9
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of -Secretase.
Amgen
39
Purinylpyridinylamino-based DFG-in/aC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.
Amgen
161
Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.
Amgen
34
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Amgen
13
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
Amgen
6
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.
Amgen
15
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.
Amgen
54
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.
Amgen
3
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Amgen
2
Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.
Amgen
3
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
Amgen
1
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
Amgen
70
Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Amgen
20
Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Amgen
26
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Amgen
9
Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease.
Amgen
19
An Orally Available BACE1 Inhibitor That Affords Robust CNS A Reduction without Cardiovascular Liabilities.
Amgen
26
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.
Amgen
21
Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious -secretase inhibitors for the potential treatment of Alzheimer's disease.
Amgen
31
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Amgen
45
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.
Amgen
33
Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
19
Unfolded Protein Response in Cancer: IRE1a Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability.
Amgen
26
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Amgen
21
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.
Amgen
36
Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene -site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Amgen
18
Inhibitors of -site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).
Amgen
18
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
Amgen
33
Structure-assisted discovery of the first non-retinoid ligands for Retinol-Binding Protein 4.
Amgen
10
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
Amgen
52
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
Amgen
40
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
Amgen
47
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Amgen
28
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Amgen
23
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
45
Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents.
Amgen
30
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Amgen
46
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Amgen
24
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
Amgen
48
Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists.
Amgen
31
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
Amgen
2
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
21
Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists.
Amgen
3
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
21
Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism.
Amgen
21
Discovery of 2-methylpyridine-based biaryl amides as -secretase modulators for the treatment of Alzheimer's disease.
Amgen
22
Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.
Amgen
17
Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.
Amgen
31
Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.
Amgen
23
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Amgen
5
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
31
Inhibiting NF-¿B-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.
Amgen
38
Discovery of INT131: a selective PPAR¿ modulator that enhances insulin sensitivity.
Amgen
4
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.
Amgen
45
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.
Amgen
15
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.
Amgen
22
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Amgen
2
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
Amgen
37
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.
Amgen
31
Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Amgen
13
Design and preparation of a potent series of hydroxyethylamine containingß-secretase inhibitors that demonstrate robust reduction of centralß-amyloid.
Amgen
20
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Amgen
35
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Amgen
37
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Amgen
26
Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Amgen
57
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Amgen
35
Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.
Amgen
15
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1¿) inhibitors.
Amgen
4
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
Amgen
26
Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction.
Amgen
37
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11ß-HSD1 inhibitors.
Amgen
16
Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
Amgen
8
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.
Amgen
49
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Amgen
11
Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
Amgen
48
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
36
Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.
Amgen
32
Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.
Amgen
57
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.
Amgen
41
The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.
Amgen
16
Fragment based drug discovery: practical implementation based on¹¿F NMR spectroscopy.
Amgen
13
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.
Amgen
23
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Amgen
11
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
Amgen
44
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Amgen
46
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Amgen
24
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Amgen
23
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
Amgen
21
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
12
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
Amgen
10
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Amgen
46
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
Amgen
83
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Amgen
5
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Amgen
42
Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.
Amgen
16
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
Amgen
26
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups.
Amgen
1
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
Amgen
26
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Amgen
56
Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency.
Amgen
20
Quinolinone-based agonists of S1P¿?: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Amgen
17
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P¿? agonists with in vivo lymphocyte-depleting activity.
Amgen
20
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.
Amgen
29
Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2.
Amgen
20
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
Amgen
23
Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Amgen
39
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Amgen
32
Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.
Amgen
20
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Amgen
35
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.
Amgen
17
Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.
Amgen
36
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Amgen
39
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
38
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Amgen
61
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
Amgen
61
Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition.
Amgen
27
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
38
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Amgen
18
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11ß-HSD1 inhibitors.
Amgen
23
Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors.
Amgen
14
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
18
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Amgen
27
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Amgen
16
Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.
Amgen
8
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Amgen
12
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.
Amgen
17
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
23
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
36
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
85
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Amgen
14
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Amgen
8
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Amgen
18
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
Amgen
28
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
16
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Amgen
25
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.
Amgen
33
Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Amgen
38
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Amgen
31
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
Amgen
11
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Amgen
17
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
20
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Amgen
2
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Amgen
13
Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
Amgen
19
Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
Amgen
25
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Amgen
16
Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists.
Amgen
5
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
Amgen
26
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
22
Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation.
Amgen
17
Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties.
Amgen
16
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.
Amgen
19
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
Amgen
21
Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Amgen
25
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Amgen
21
Identification of Structurally Novel KRASG12C Inhibitors through Covalent DNA-Encoded Library Screening.
Amgen
9
From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy.
Amgen
28
Discovery of AMG 193, an MTA-Cooperative PRMT5 Inhibitor for the Treatment of MTAP-Deleted Cancers.
Amgen
12
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Amgen
27
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Amgen
18
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Amgen
35
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Amgen
18
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Amgen
19
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Amgen
16
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
Amgen
33
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Amgen
34
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
24
Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.
Amgen
26
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Amgen
3
Discovery of Selective Pituitary Adenylate Cyclase 1 Receptor (PAC1R) Antagonist Peptides Potent in a Maxadilan/PACAP38-Induced Increase in Blood Flow Pharmacodynamic Model.
Amgen
36
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Amgen
28
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Amgen
53
SAR and mode of action of novel non-nucleoside inhibitors of hepatitis C NS5b RNA polymerase.
Amgen
27
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
Amgen
15
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Amgen
64
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Amgen
19
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Amgen
16
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.
Amgen
15
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.
Amgen
14
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Amgen
22
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Amgen
40
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.
Amgen
95
Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.
Amgen
26
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Amgen
5
Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.
Amgen
37
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
Amgen
27
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Amgen
25
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.
Amgen
24
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Amgen
19
Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4.
Amgen
3
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
Amgen
6
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Amgen
17
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Amgen
170
Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.
Amgen
18
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Amgen
17
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
Amgen
5
Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine β-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation.
Amgen
16
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na
Amgen
627
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
Amgen
274
Heterocyclic compounds as delta-5 desaturase inhibitors and methods of use
Amgen
71
QUINAZOLINE COMPOUNDS AND USES THEREOF AS INHIBITORS OF MUTANT KRAS PROTEINS
Amgen
576
Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use
Amgen
35
EPOXYAMIDES AS KRAS G12C AND KRAS G12D INHIBITORS AND METHODS OF USING THE SAME
Amgen
46
Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
Amgen
80
CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
Amgen
171
Alpha-hydroxy phenylacetic acid pharmacophore or bioisostere Mcl-1 protein antagonists
Amgen
166
1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
Amgen
115
Cycloalkyl substituted triazole compounds as agonists of the APJ receptor
Amgen
40
Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
Amgen
248
Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
Amgen
7
Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
Amgen
399
Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
Amgen
224
Compounds for use in preparing heterocyclic triazole agonists of the APJ receptor
Amgen
168
Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
Amgen
10
5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
Amgen
93
Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
Amgen
230
Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
Amgen
11
Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
Amgen
29
Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
Amgen
480
Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
Amgen
21
Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
Amgen
351
Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
Amgen
21
Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1a prolyl hydroxylases-1, -2, and -3 with altered selectivity.
Amgen
6
Cloning and functional expression of cDNAs encoding human and rat pancreatic polypeptide receptors.
Amgen
12
Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.
Amgen
46
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).
Amgen
29
Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Amgen
15
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.
Amgen
26
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
Amgen
1
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.
Amgen
18
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
Amgen
8
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Amgen
18
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.
Amgen
33
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Amgen
26
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Amgen
24
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Amgen
29
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Amgen
23
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Amgen
22
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Amgen
11
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.
Amgen
36
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.
Amgen
35
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
Amgen
23
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
Amgen