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Systematic Study of the Glutathione Reactivity of N‑Phenylacrylamides: 2. Effects of Acrylamide Substitution

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11602-11614

2020

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Curcuminoids inhibit multiple human cytochromes P450, UDP-glucuronosyltransferase, and sulfotransferase enzymes, whereas piperine is a relatively selective CYP3A4 inhibitor

Drug metabolism and disposition, 2008-08, Vol.36 (8), p.1594-1605

2008

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Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers

British journal of clinical pharmacology, 2013-02, Vol.75 (2), p.450-462

2013

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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

Nature (London), 2019-11, Vol.575 (7781), p.217-223

2019

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Industry Perspective on the Pharmacokinetic and Absorption, Distribution, Metabolism, and Excretion Characterization of Heterobifunctional Protein Degraders

Drug metabolism and disposition, 2023-07, Vol.51 (7), p.792-803

2023

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Systematic Study of the Glutathione (GSH) Reactivity of N‑Arylacrylamides: 1. Effects of Aryl Substitution

Journal of medicinal chemistry, 2015-12, Vol.58 (23), p.9171-9178

2015

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Current Approaches for Predicting Human PK for Small Molecule Development Candidates: Findings from the IQ Human PK Prediction Working Group Survey

The AAPS journal, 2022-07, Vol.24 (5), p.85-85, Article 85

2022

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Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human

Drug metabolism and disposition, 2022-08, Vol.50 (8), p.1064-1076

2022

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Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation

Proceedings of the National Academy of Sciences - PNAS, 2024-01, Vol.121 (1), p.e2307086120

2024

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Intravital Multiphoton Microscopy with Fluorescent Bile Salts in Rats as an In Vivo Biomarker for Hepatobiliary Transport Inhibition

Drug metabolism and disposition, 2018-05, Vol.46 (5), p.704-718

2018

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Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2020-01, Vol.63 (1), p.52-65

2020

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Discovery of N‑(1-Acryloylazetidin-3-yl)-2-(1H‑indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C

ACS medicinal chemistry letters, 2019-09, Vol.10 (9), p.1302-1308

2019

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Discovery of N -(1-Acryloylazetidin-3-yl)-2-(1 H -indol-1-yl)acetamides as Covalent Inhibitors of KRAS G12C

ACS medicinal chemistry letters, 2019-09, Vol.10 (9), p.1302-1308

2019

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Zinc Status Influences Zinc Transport by Porcine Brain Capillary Endothelial Cells

The Journal of nutrition, 2002-09, Vol.132 (9), p.2763-2768

2002

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Abstract 4484: Discovery and in vitro characterization of AMG 510–a potent and selective covalent small-molecule inhibitor of KRASG12C

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.4484-4484

2019

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Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.4455-4455

2019

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Characterization of JNJ-2482272 [4-(4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-yl)pyrimidine-2-amine] as a Strong AhR Activator in Rat and Human

Drug metabolism and disposition, 2022-06

2022

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Role for protein kinase C delta in the functional activity of human UGT1A6: implications for drug-drug interactions between PKC inhibitors and UGT1A6

Xenobiotica, 2010-05, Vol.40 (5), p.306-318

2010

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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2020-01, Vol.63 (1), p.52-65

2020

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Inhibition of UDP‐glucuronosyltransferase (UGT) enzymes by protein kinase C inhibitors

The FASEB journal, 2008-03, Vol.22 (S1)

2008

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Abstract C84: Nonclinical metabolism, disposition, pharmacokinetics, and in vitro drug-drug interaction assessment of ARQ 087, a pan-FGFR inhibitor

Molecular cancer therapeutics, 2013-11, Vol.12 (11_Supplement), p.C84-C84

2013

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Abstract C83: Nonclinical in vitro ADME, disposition, and pharmacokinetic assessment of ARQ 092, a selective AKT inhibitor

Molecular cancer therapeutics, 2013-11, Vol.12 (11_Supplement), p.C83-C83

2013

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Curcuminoid-piperine interaction with the major drug metabolizing enzymes: Mechanisms and consequences

Volak, Laurie P

2009

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In Vitro Approaches to Anticipating Clinical Drug Interactions

Drug–Drug Interactions in Pharmaceutical Development, 2007, p.31-74

2007

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Systematic Study of the Glutathione Reactivity of N‑Phenylacrylamides: 2. Effects of Acrylamide Substitution

Curcuminoids inhibit multiple human cytochromes P450, UDP-glucuronosyltransferase, and sulfotransferase enzymes, whereas piperine is a relatively selective CYP3A4 inhibitor

Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers

Discovery and Optimization of a Series of 3-(3-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: Orally Bioavailable, Selective, and Potent ATP-Independent Akt Inhibitors

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

Industry Perspective on the Pharmacokinetic and Absorption, Distribution, Metabolism, and Excretion Characterization of Heterobifunctional Protein Degraders

Systematic Study of the Glutathione (GSH) Reactivity of N‑Arylacrylamides: 1. Effects of Aryl Substitution

Current Approaches for Predicting Human PK for Small Molecule Development Candidates: Findings from the IQ Human PK Prediction Working Group Survey

Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human

Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation

Intravital Multiphoton Microscopy with Fluorescent Bile Salts in Rats as an In Vivo Biomarker for Hepatobiliary Transport Inhibition

Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors

Discovery of N‑(1-Acryloylazetidin-3-yl)-2-(1H‑indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C

Discovery of N -(1-Acryloylazetidin-3-yl)-2-(1 H -indol-1-yl)acetamides as Covalent Inhibitors of KRAS G12C

Zinc Status Influences Zinc Transport by Porcine Brain Capillary Endothelial Cells

Abstract 4484: Discovery and in vitro characterization of AMG 510–a potent and selective covalent small-molecule inhibitor of KRASG12C

Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors

Characterization of JNJ-2482272 [4-(4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-yl)pyrimidine-2-amine] as a Strong AhR Activator in Rat and Human

Role for protein kinase C delta in the functional activity of human UGT1A6: implications for drug-drug interactions between PKC inhibitors and UGT1A6

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

Inhibition of UDP‐glucuronosyltransferase (UGT) enzymes by protein kinase C inhibitors

Abstract C84: Nonclinical metabolism, disposition, pharmacokinetics, and in vitro drug-drug interaction assessment of ARQ 087, a pan-FGFR inhibitor

Abstract C83: Nonclinical in vitro ADME, disposition, and pharmacokinetic assessment of ARQ 092, a selective AKT inhibitor

Curcuminoid-piperine interaction with the major drug metabolizing enzymes: Mechanisms and consequences

In Vitro Approaches to Anticipating Clinical Drug Interactions

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