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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50384609
Substrate
n/a
Meas. Tech.
ChEMBL_820659 (CHEMBL2037930)
IC50
10±n/a nM
Citation
 Liu, J; Yang, C; Simpson, C; Deryckere, D; Van Deusen, A; Miley, MJ; Kireev, D; Norris-Drouin, J; Sather, S; Hunter, D; Korboukh, VK; Patel, HS; Janzen, WP; Machius, M; Johnson, GL; Earp, HS; Graham, DK; Frye, SV; Wang, X Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett 3:129-134 (2012) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Mer
Synonyms:
MER | MER intracellular domain/EGFR extracellular domain chimera | MERTK | MERTK_HUMAN | Proto-oncogene c-Mer | Proto-oncogene tyrosine-protein kinase MER | Receptor tyrosine kinase MerTK | Tyrosine-protein kinase Mer
Type:
PROTEIN
Mol. Mass.:
110234.77
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1498723
Residue:
999
Sequence:
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQPALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVPNIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKINNEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNEQPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSILISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVSCMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGYRISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFIPAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTEEDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMSSQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPDSIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGERLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
  
Inhibitor
Name:
BDBM50384609
Synonyms:
CHEMBL2036802 | US9744172, Compound UNC00000546A
Type:
Small organic molecule
Emp. Form.:
C26H30N6O
Mol. Mass.:
442.556
SMILES:
COc1ccc(CNc2ncc3c(nn(CC4CCC(N)CC4)c3n2)-c2ccccc2)cc1 |(30.43,6.19,;29.1,5.42,;29.1,3.88,;30.43,3.11,;30.43,1.57,;29.09,.81,;29.09,-.73,;30.43,-1.5,;31.76,-.74,;31.76,.81,;33.09,1.58,;34.43,.82,;35.9,1.3,;36.81,.04,;35.9,-1.21,;36.38,-2.68,;35.35,-3.82,;33.84,-3.49,;32.81,-4.63,;33.28,-6.1,;32.24,-7.24,;34.79,-6.42,;35.83,-5.28,;34.43,-.74,;33.09,-1.51,;36.38,2.76,;37.88,3.08,;38.36,4.54,;37.33,5.69,;35.82,5.36,;35.35,3.9,;27.77,1.57,;27.76,3.1,)|
Structure:
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