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Target
Tyrosine-protein kinase receptor Tie-1
Ligand
BDBM50384727
Substrate
n/a
Meas. Tech.
ChEMBL_821006 (CHEMBL2039193)
IC50
5700±n/a nM
Citation
 Albaugh, P; Fan, Y; Mi, Y; Sun, F; Adrian, F; Li, N; Jia, Y; Sarkisova, Y; Kreusch, A; Hood, T; Lu, M; Liu, G; Huang, S; Liu, Z; Loren, J; Tuntland, T; Karanewsky, DS; Seidel, HM; Molteni, V Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS Med Chem Lett 3:140-145 (2012) [PubMed]  Article
Target
Name:
Tyrosine-protein kinase receptor Tie-1
Synonyms:
TIE1_MOUSE | Tie | Tie-1 | Tie1
Type:
PROTEIN
Mol. Mass.:
124588.36
Organism:
Mus musculus
Description:
ChEMBL_821006
Residue:
1134
Sequence:
MVWWGSSLLLPTLFLASHVGASVDLTLLANLRITDPQRFFLTCVSGEAGAGRSSDPPLLLEKDDRIVRTFPPGQPLYLARNGSHQVTLRGFSKPSDLVGVFSCVGGAGARRTRVLYVHNSPGAHLFPDKVTHTVNKGDTAVLSAHVHKEKQTDVIWKNNGSYFNTLDWQEADDGRFQLQLQNVQPPSSGIYSATYLEASPLGSAFFRLIVRGCGAGRWGPGCVKDCPGCLHGGVCHDHDGECVCPPGFTGTRCEQACREGRFGQSCQEQCPGTAGCRGLTFCLPDPYGCSCGSGWRGSQCQEACAPGHFGADCRLQCQCQNGGTCDRFSGCVCPSGWHGVHCEKSDRIPQILSMATEVEFNIGTMPRINCAAAGNPFPVRGSMKLRKPDGTMLLSTKVIVEPDRTTAEFEVPSLTLGDSGFWECRVSTSGGQDSRRFKVNVKVPPVPLTAPRLLAKQSRQLVVSPLVSFSGDGPISSVRLHYRPQDSTIAWSAIVVDPSENVTLMNLKPKTGYNVRVQLSRPGEGGEGGWGPSALMTTDCPEPLLQPWLESWHVEGPDRLRVSWSLPSVPLSGDGFLLRLWDGARGQERRENISFPQARTALLTGLTPGTHYQLDVRLYHCTLLGPASPPAHVHLPPSGPPAPRHLHAQALSDSEIQLMWQHPEAPSGPISKYIVEIQVAGGSGDPQWMDVDRPEETSIIVRGLNASTRYLFRVRASVQGLGDWSNTVEEATLGNGLQSEGPVRESRAAEEGLDQQLVLAVVGSVSATCLTILAALLALVCIRRSCLHRRRTFTYQSGSGEETILQFSSGTLTLTRRPKPQPEPLSYPVLEWEDITFEDLIGEGNFGQVIRAMIKKDGLKMNAAIKMLKEYASENDHRDFAGELEVLCKLGHHPNIINLLGACENRGYLYIAIEYAPYGNLLDFLRKSRVLETDPAFAREHGTASTLSSRQLLRFASDAANGMQYLSEKQFIHRDLAARNVLVGENLASKIADFGLSRGEEVYVKKTMGRLPVRWMAIESLNYSVYTTKSDVWSFGVLLWEIVSLGGTPYCGMTCAELYEKLPQGYRMEQPRNCDDEVYELMRQCWRDRPYERPPFAQIALQLGRMLEARKAYVNMSLFENFTYAGIDATAEEA
  
Inhibitor
Name:
BDBM50384727
Synonyms:
CHEMBL2037226
Type:
Small organic molecule
Emp. Form.:
C28H21F4N5O2
Mol. Mass.:
535.4923
SMILES:
Cc1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)cc1Nc1ccc2\C(=C\c3ccc[nH]3)C(=O)Nc2c1
Structure:
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