Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.

PTW, Cheng; RF 3rd, Kaltenbach; H, Zhang; J, Shi; S, Tao; J, Li; LJ, Kennedy; SJ, Walker; Y, Shi; Y, Wang; S, Dhanusu; R, Reddigunta; S, Kumaravel; S, Jusuf; D, Smith; S, Krishnananthan; J, Li; T, Wang; R, Heiry; CS, Sum; SS, Kalinowski; CP, Hung; CH, Chu; AV, Azzara; M, Ziegler; L, Burns; BA, Zinker; S, Boehm; J, Taylor; J, Sapuppo; K, Mosure; G, Everlof; V, Guarino; L, Zhang; Y, Yang; Q, Ruan; C, Xu; A, Apedo; SC, Traeger; ME, Cvijic; KA, Lentz; G, Tirucherai; L, Sivaraman; J, Robl; BA, Ellsworth; G, Rosen; DA, Gordon; MG, Soars; M, Gill; BJ, Murphy

doi:10.1021/acs.jmedchem.1c01256

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Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.

Shared by NobleBlocks on Oct 28, 2021 • 12:00 AM UTC

Authors:

Cheng PTW

Kaltenbach RF 3rd

Zhang H

Abstract

The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA1 antagonist clinical compound BMS-9...

Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA<sub>1</sub>) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.

Abstract

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