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TitleDiscovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.
Journal, issue, pagesJ. Med. Chem., Vol. 67, Page 17000-17032, Year 2024
Publish dateApr 20, 2024 (structure data deposition date)
AuthorsYu, Y. / Jang, M. / Miyashiro, J. / Clark, R.F. / Zhu, G.D. / Gong, J. / Dai, Y. / Frey, R.R. / Penning, T.D. / Kim, H. ...Yu, Y. / Jang, M. / Miyashiro, J. / Clark, R.F. / Zhu, G.D. / Gong, J. / Dai, Y. / Frey, R.R. / Penning, T.D. / Kim, H. / Lee, H.K. / Kim, J.K. / Ryu, K.M. / Park, S.J. / Yoon, T. / Li, T. / Kurnick, M.D. / Kapecki, N.J. / Li, L. / Gorman, J.V. / Montgomery, D.A. / Manaves, V. / Bromberg, K.D. / Doktor, S.Z. / Thakur, A. / Wang, J. / Smith, H.A. / Buchanan, F.G. / Ferguson, D.C. / Torrent, M. / Jakob, C.G. / Qiu, W. / Upadhyay, A.K. / Martin, R.L. / Lai, A. / Michaelides, M.R.
External linksJ. Med. Chem. / PubMed:39283694
MethodsX-ray diffraction
Resolution2.07 Å
Structure data

PDB-9bhi:
Crystal structure of the MerTK kinase domain with SA4488
Method: X-RAY DIFFRACTION / Resolution: 2.07 Å

Chemicals

PDB-1apf:
ANTHOPLEURIN-B, NMR, 20 STRUCTURES

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Receptor Tyrosine Kinase / ATP competitive inhibitor

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