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Drug Metabolism & Disposition

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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

Kevin J. Coe, Mark Feinstein, J. William Higgins, Perry Leung, Brian P Scott, Judith Skaptason, Yuen Tam, Laurie P Volak, Jennifer Kinong, Anton Bittner, Heather McAllister, Nathan M Lim, Michael Hack and Tatiana Koudriakova
Drug Metabolism and Disposition June 9, 2022, DMD-AR-2021-000825; DOI: https://doi.org/10.1124/dmd.121.000825
Kevin J. Coe
1DMPK, Janssen Research & Development, United States
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  • ORCID record for Kevin J. Coe
  • For correspondence: kcoe2@its.jnj.com
Mark Feinstein
1DMPK, Janssen Research & Development, United States
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J. William Higgins
2Trestle Biotherapeutics, United States
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Perry Leung
3Janssen Research & Development, United States
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Brian P Scott
1DMPK, Janssen Research & Development, United States
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Judith Skaptason
4DMPK, Neurocrine Biosciences, Inc., United States
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Yuen Tam
1DMPK, Janssen Research & Development, United States
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Laurie P Volak
3Janssen Research & Development, United States
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Jennifer Kinong
5Pfizer, United States
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Anton Bittner
6Turnstone Biologics, United States
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Heather McAllister
3Janssen Research & Development, United States
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Nathan M Lim
3Janssen Research & Development, United States
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Michael Hack
3Janssen Research & Development, United States
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Tatiana Koudriakova
1DMPK, Janssen Research & Development, United States
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    • Supplemental Data  -

      Supplemental Figure S1: Cell Viability Studies in Plated Rat Hepatocytes.

      Supplemental Figure S2: Proton NMR Spectrum of JNJ-2482272.

      Supplemental Figure S3: Proton NMR Spectrum of M4.

      Supplemental Figure S4: Proton NMR Spectrum of M5.

      Supplemental Figure S5: Cell Viability Studies in Human Reporter Cell Lines.

      Supplemental Figure S6: Induction of P450 Gene Expression in Pooled Human Donor Hepatocytes.

       Supplemental Figure S7: Induction of CYP1A and CYP3A Activity in Pooled Human Donor Hepatocytes.

      Supplemental Figure S8: Quantum Mechanic Dihedral Scan of JNJ-2482272.

      Supplemental Table S1: Cell Viability Studies in Plated Primary Human Hepatocytes

      Supplemental Table S2: JNJ-2482272 P450 Inhibition in Human Liver Microsomes

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Drug Metabolism and Disposition: 50 (6)
Drug Metabolism and Disposition
Vol. 50, Issue 6
1 Jun 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 AhR Activator in Rat and Human
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Metabolism and AhR Activation of JNJ-2482272

Kevin J. Coe, Mark Feinstein, J. William Higgins, Perry Leung, Brian P Scott, Judith Skaptason, Yuen Tam, Laurie P Volak, Jennifer Kinong, Anton Bittner, Heather McAllister, Nathan M Lim, Michael Hack and Tatiana Koudriakova
Drug Metabolism and Disposition June 9, 2022, DMD-AR-2021-000825; DOI: https://doi.org/10.1124/dmd.121.000825

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OtherArticle

Metabolism and AhR Activation of JNJ-2482272

Kevin J. Coe, Mark Feinstein, J. William Higgins, Perry Leung, Brian P Scott, Judith Skaptason, Yuen Tam, Laurie P Volak, Jennifer Kinong, Anton Bittner, Heather McAllister, Nathan M Lim, Michael Hack and Tatiana Koudriakova
Drug Metabolism and Disposition June 9, 2022, DMD-AR-2021-000825; DOI: https://doi.org/10.1124/dmd.121.000825
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