Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase kinase kinase kinase 4
Ligand
BDBM50308060
Substrate
n/a
Meas. Tech.
ChEMBL_655452 (CHEMBL1244496)
Kd
23±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 4
Synonyms:
HGK | HPK/GCK-like kinase HGK | KIAA0687 | M4K4_HUMAN | MAP4K4 | MAP4K4 (HGK) | MAPK/ERK kinase kinase kinase 4 | MEK kinase kinase 4 | MEKKK 4 | Mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) | NIK | Nck-interacting kinase
Type:
Serine/threonine-protein kinase
Mol. Mass.:
142114.73
Organism:
Homo sapiens (Human)
Description:
O95819
Residue:
1239
Sequence:
MANDSPAKSLVDIDLSSLRDPAGIFELVEVVGNGTYGQVYKGRHVKTGQLAAIKVMDVTEDEEEEIKLEINMLKKYSHHRNIATYYGAFIKKSPPGHDDQLWLVMEFCGAGSITDLVKNTKGNTLKEDWIAYISREILRGLAHLHIHHVIHRDIKGQNVLLTENAEVKLVDFGVSAQLDRTVGRRNTFIGTPYWMAPEVIACDENPDATYDYRSDLWSCGITAIEMAEGAPPLCDMHPMRALFLIPRNPPPRLKSKKWSKKFFSFIEGCLVKNYMQRPSTEQLLKHPFIRDQPNERQVRIQLKDHIDRTRKKRGEKDETEYEYSGSEEEEEEVPEQEGEPSSIVNVPGESTLRRDFLRLQQENKERSEALRRQQLLQEQQLREQEEYKRQLLAERQKRIEQQKEQRRRLEEQQRREREARRQQEREQRRREQEEKRRLEELERRRKEEEERRRAEEEKRRVEREQEYIRRQLEEEQRHLEVLQQQLLQEQAMLLECRWREMEEHRQAERLQRQLQQEQAYLLSLQHDHRRPHPQHSQQPPPPQQERSKPSFHAPEPKAHYEPADRAREVEDRFRKTNHSSPEAQSKQTGRVLEPPVPSRSESFSNGNSESVHPALQRPAEPQVPVRTTSRSPVLSRRDSPLQGSGQQNSQAGQRNSTSIEPRLLWERVEKLVPRPGSGSSSGSSNSGSQPGSHPGSQSGSGERFRVRSSSKSEGSPSQRLENAVKKPEDKKEVFRPLKPADLTALAKELRAVEDVRPPHKVTDYSSSSEESGTTDEEDDDVEQEGADESTSGPEDTRAASSLNLSNGETESVKTMIVHDDVESEPAMTPSKEGTLIVRQTQSASSTLQKHKSSSSFTPFIDPRLLQISPSSGTTVTSVVGFSCDGMRPEAIRQDPTRKGSVVNVNPTNTRPQSDTPEIRKYKKRFNSEILCAALWGVNLLVGTESGLMLLDRSGQGKVYPLINRRRFQQMDVLEGLNVLVTISGKKDKLRVYYLSWLRNKILHNDPEVEKKQGWTTVGDLEGCVHYKVVKYERIKFLVIALKSSVEVYAWAPKPYHKFMAFKSFGELVHKPLLVDLTVEEGQRLKVIYGSCAGFHAVDVDSGSVYDIYLPTHIQCSIKPHAIIILPNTDGMELLVCYEDEGVYVNTYGRITKDVVLQWGEMPTSVAYIRSNQTMGWGEKAIEIRSVETGHLDGVFMHKRAQRLKFLCERNDKVFFASVRSGGSSQVYFMTLGRTSLLSW
  
Inhibitor
Name:
BDBM50308060
Synonyms:
16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one | CEP-701 | CHEMBL603469 | US11370779, Compound CEP-701
Type:
Small organic molecule
Emp. Form.:
C26H21N3O4
Mol. Mass.:
439.4626
SMILES:
C[C@]12O[C@H](C[C@]1(O)CO)n1c3ccccc3c3c4C(=O)NCc4c4c5ccccc5n2c4c13 |r|
Structure:
Search PDB for entries with ligand similarity: