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Target
Tyrosine-protein kinase Mer
Ligand
BDBM246866
Substrate
n/a
Meas. Tech.
TAM Kinase Assay
Temperature
298.15±n/a K
IC50
<500±n/a nM
Comments
extracted
Citation
 Li, Y; Burns, DM; Feng, H; Glenn, J; He, C; Huang, T; Mei, S; Pan, J; Wang, X; Ye, Y Pyrrolopyrimidine derivatives as TAM inhibitors US Patent  US10053465 Publication Date 8/21/2018 
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:
BDBM246866
Synonyms:
4-[(4-{3-cyano-2-[4- (7H-pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]propyl}piperazin- 1-yl)carbonyl]-3- fluorobenzonitrile | US10053465, 5 | US10065963, Compound 5 | US10125150, Example 5 | US11084822, Example 5
Type:
Small organic molecule
Emp. Form.:
C25H22FN9O
Mol. Mass.:
483.5003
SMILES:
Fc1cc(ccc1C(=O)N1CCN(CC(CC#N)n2cc(cn2)-c2ncnc3[nH]ccc23)CC1)[N+]#[C-]
Structure:
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