| Parameter | Value (mouse) | Value (rat) | Value (dog) | |-----------|---------------|-------------|-------------| | (LPA₅ functional antagonism, Ca²⁺ flux) | 42 nM | 48 nM | 55 nM | | Selectivity (≥ 100‑fold vs. LPA₁‑₄, S1P₁‑₅) | — | — | — | | Oral bioavailability | 68 % (p.o., 10 mg kg⁻¹) | 62 % | 55 % | | C_max (μM) at 30 mg kg⁻¹ p.o. | 4.2 | 3.8 | 3.1 | | t₁/₂ (h) | 3.5 | 4.2 | 5.0 | | Plasma protein binding | 92 % (mouse) | 90 % (rat) | 88 % (dog) | | Brain penetration (K_p,uu) | 0.12 | 0.09 | 0.07 | | Key metabolites | N‑desethyl MEYD‑873 (inactive) | N‑desethyl (inactive) | Same |
The mitogen‑activated protein kinase (MAPK) family consists of four major branches: ERK1/2, JNK, p38, and ERK5 (also known as BMK1). While ERK1/2 has long been the focus of oncology drug discovery, ERK5 has emerged over the past decade as an equally compelling target. ERK5 uniquely couples a kinase domain (KD) to a large C‑terminal transcriptional activation domain (TAD), enabling dual regulation of cytoplasmic signaling and nuclear gene expression. MEYD-873
The compound exhibits low CNS exposure, consistent with the intended peripheral therapeutic window. | Parameter | Value (mouse) | Value (rat)
The following essay presents a deep‑dive analysis of MEYD‑873, covering its discovery, chemical attributes, pharmacological properties, development trajectory, and the strategic considerations that shape its future as a potential first‑in‑class therapeutic. While ERK1/2 has long been the focus of
Author: ChatGPT, Ph.D. (Synthetic Chemistry & Drug Development) Date: 9 April 2026