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Target
Tyrosine-protein kinase Mer
Ligand
BDBM497300
Substrate
n/a
Meas. Tech.
ChEMBL_2129273 (CHEMBL4838702)
IC50
9.5±n/a nM
Citation
 Zheng, H; Zhao, J; Li, B; Zhang, W; Stashko, MA; Minson, KA; Huey, MG; Zhou, Y; Earp, HS; Kireev, D; Graham, DK; DeRyckere, D; Frye, SV; Wang, X UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem 220:0 (2021) [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:
BDBM497300
Synonyms:
(4- (dimethylamino)phenyl)(4- (7-((1r,4S)-4- hydroxycyclohexyl)-2- (((S)-pentan-2-yl)amino)- 7H-pyrrolo[2,3- d]pyrimidin-5-yl)piperidin- 1-yl)methanone | US11001586, Example 79
Type:
Small organic molecule
Emp. Form.:
C31H44N6O2
Mol. Mass.:
532.7201
SMILES:
CCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)C1CCN(CC1)C(=O)c1ccc(cc1)N(C)C |r,wU:13.12,wD:16.16,3.3,(-9.88,-2.91,;-8.55,-2.14,;-7.21,-2.91,;-5.88,-2.14,;-5.88,-.6,;-4.55,-2.91,;-3.21,-2.14,;-3.21,-.6,;-1.88,.17,;-.54,-.6,;.92,-.13,;1.83,-1.37,;.92,-2.62,;1.4,-4.08,;2.9,-4.4,;3.38,-5.87,;2.35,-7.01,;2.82,-8.48,;.84,-6.69,;.37,-5.23,;-.54,-2.14,;-1.88,-2.91,;1.4,1.34,;2.9,1.66,;3.38,3.12,;2.35,4.27,;.84,3.95,;.37,2.48,;2.82,5.73,;1.79,6.88,;4.33,6.05,;5.36,4.91,;6.87,5.23,;7.34,6.69,;6.31,7.84,;4.81,7.52,;8.85,7.01,;9.88,5.87,;9.33,8.48,)|
Structure:
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