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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50444265
Substrate
n/a
Meas. Tech.
ChEMBL_1277932 (CHEMBL3094776)
IC50
120±n/a nM
Citation
 Zhang, W; McIver, AL; Stashko, MA; DeRyckere, D; Branchford, BR; Hunter, D; Kireev, D; Miley, MJ; Norris-Drouin, J; Stewart, WM; Lee, M; Sather, S; Zhou, Y; Di Paola, JA; Machius, M; Janzen, WP; Earp, HS; Graham, DK; Frye, SV; Wang, X Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem 56:9693-700 (2014) [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:
BDBM50444265
Synonyms:
CHEMBL3093633
Type:
Small organic molecule
Emp. Form.:
C28H33FN6O5S
Mol. Mass.:
584.662
SMILES:
O[C@H]1CC[C@@H](CC1)Nc1nc(NCc2ccc(F)cc2)ncc1C(=O)Nc1ccc(cc1)S(=O)(=O)N1CCOCC1 |r,wU:4.7,wD:1.0,(51.68,-38.67,;53.01,-39.44,;53.01,-40.98,;54.35,-41.76,;55.67,-40.99,;55.67,-39.44,;54.35,-38.68,;57.01,-41.75,;57.01,-43.29,;55.69,-44.06,;55.68,-45.61,;54.35,-46.38,;53.02,-45.61,;51.68,-46.37,;50.36,-45.59,;49.03,-46.36,;49.02,-47.9,;47.68,-48.66,;50.35,-48.67,;51.69,-47.91,;57.02,-46.38,;58.35,-45.61,;58.35,-44.06,;59.68,-43.28,;59.67,-41.74,;61.02,-44.05,;62.35,-43.27,;63.68,-44.04,;65.01,-43.27,;65,-41.73,;63.66,-40.96,;62.33,-41.74,;66.33,-40.95,;65.56,-39.61,;67.1,-39.6,;67.67,-41.71,;67.67,-43.25,;69,-44.01,;70.33,-43.24,;70.33,-41.7,;68.99,-40.93,)|
Structure:
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