General Information of the Protein
Protein ID
PT07205
Protein Name
Tyrosine-protein kinase Mer
Secondarily
Protein Name
Proto-oncogene c-Mer
Receptor tyrosine kinase MerTK
Gene Name
MERTK
Secondarily
Gene Name
Mer
Sequence
MVLAPLLLGLLLLPALWSGGTAEKWEETELDQLFSGPLPGRLPVNHRPFSAPHSSRDQLPPPQTGRSHPAHTAAPQVTSTASKLLPPVAFNHTIGHIVLSEHKNVKFNCSINIPNTYQETAGISWWKDGKELLGAHHSITQFYPDEEGVSIIALFSIASVQRSDNGSYFCKMKVNNREIVSDPIYVEVQGLPYFIKQPESVNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNEKPERSPSVLTVPGLTETAVFSCEAHNDKGLTVSKGVHINIKVIPSPPTEVHILNSTAHSILVSWVPGFDGYSPLQNCSIQVKEADRLSNGSVMVFNTSASPHLYEIQQLQALANYSIAVSCRNEIGWSAVSPWILASTTEGAPSVAPLNITVFLNESNNILDIRWTKPPIKRQDGELVGYRISHVWESAGTYKELSEEVSQNGSWAQIPVQIHNATCTVRIAAITKGGIGPFSEPVNIIIPEHSKVDYAPSSTPAPGNTDSMFIILGCFCGFILIGLILCISLALRRRVQETKFGGAFSEEDSQLVVNYRAKKSFCRRAIELTLQSLGVSEELQNKLEDVVIDRNLLVLGKVLGEGEFGSVMEGNLKQEDGTSQKVAVKTMKLDNFSQREIEEFLSEAACMKDFNHPNVIRLLGVCIELSSQGIPKPMVILPFMKYGDLHTFLLYSRLNTGPKYIHLQTLLKFMMDIAQGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWAFGVTMWEITTRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYDIMYSCWSADPLDRPTFSVLRLQLEKLSESLPDAQDKESIIYINTQLLESCEGIANGPSLTGLDMNIDPDSIIASCTPGAAVSVVTAEVHENNLREERYILNGGNEEWEDVSSTPFAAVTPEKDGVLPEDRLTKNGVSWSHHSTLPLGSPSPDELLFVDDSLEDSEVLM
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Transferase
Function
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6. Regulates many physiological processes including cell survival, migration, differentiation, and phagocytosis of apoptotic cells (efferocytosis). Ligand binding at the cell surface induces autophosphorylation of MERTK on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signaling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganization and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Also plays an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.
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Uniprot ID
Primary ID:
Q60805

Secondarily ID:
Q62194
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Ensembl ID
ENSG00000153208
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0365521
N-[3-fluoro-4-[[7-(1-methylazetidin-3-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C31H31F2N7O4
 1
1
IC50 = 24 nM
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CP0365520
N-[4-[[6-(cyclopropanecarbonyl)-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C30H26F2N6O5
 1
1
IC50 = 34 nM
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CP0553459
1-cyclopentyl-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C36H39F2N7O4
 1
1
IC50 = 34 nM
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CP0563698
N-[3-fluoro-4-[[6-[2-(1-methylpiperidin-4-yl)acetyl]-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C34H35F2N7O5
 1
1
IC50 = 39 nM
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CP0550346
1-(cyclopropylmethyl)-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C35H37F2N7O4
 1
1
IC50 = 51 nM
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CP0569553
N-[3-fluoro-4-[[7-(1-methylpiperidin-4-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H35F2N7O4
 1
1
IC50 = 55 nM
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CP0553500
3-(4-fluorophenyl)-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C35H40FN9O5
 1
1
IC50 = 61 nM
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CP0491412
N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C34H37F2N7O4
 1
1
IC50 = 78 nM
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CP0550345
N-[4-[[7-[1-(cyclopropylmethyl)piperidin-4-yl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C36H39F2N7O4
 1
1
IC50 = 79 nM
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CP0572087
N-[3-fluoro-4-[[6-[(1-methylpiperidin-4-yl)methyl]-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H35F2N7O4
 1
1
IC50 = 80 nM
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CP0368963
N-[3-fluoro-4-[[7-[(1-methylazetidin-3-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C32H33F2N7O4
 1
1
IC50 = 92 nM
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CP0539200
N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-1-(2-methylpropyl)-2,4-dioxopyrimidine-5-carboxamide
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C35H39F2N7O4
 1
1
IC50 = 110 nM
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CP0553458
N-[3-fluoro-4-[[6-[2-(4-methylpiperazin-1-yl)acetyl]-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H34F2N8O5
 1
1
IC50 = 110 nM
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CP0562289
1-(2-fluoroethyl)-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C33H34F3N7O4
 1
1
IC50 = 130 nM
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CP0568458
1-(cyclobutylmethyl)-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C36H39F2N7O4
 1
1
IC50 = 130 nM
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CP0562288
N-[3-fluoro-4-[[7-[2-(1-methylpiperidin-4-yl)acetyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C35H37F2N7O5
 1
1
IC50 = 150 nM
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CP0563696
1-cyclopentyl-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(5-methylpyridin-2-yl)-2,4-dioxopyrimidine-5-carboxamide
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C36H41FN8O4
 1
1
IC50 = 180 nM
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CP0550347
1-(cyclopropylmethyl)-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(5-methylpyridin-2-yl)-2,4-dioxopyrimidine-5-carboxamide
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C35H39FN8O4
 1
1
IC50 = 210 nM
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CP0550344
N-[3-fluoro-4-[[6-(oxan-4-ylmethyl)-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C32H32F2N6O5
 1
1
IC50 = 240 nM
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CP0539198
N-[3-fluoro-4-[(6-oxo-5,7-dihydropyrrolo[2,3-d]pyrimidin-4-yl)oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C26H20F2N6O5
 1
1
IC50 = 280 nM
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CP0568643
3-(4-fluorophenyl)-N-[3-fluoro-4-[[6-(3-pyrrolidin-1-ylpropanoyl)-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H33F2N7O5
 1
1
IC50 = 280 nM
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CP0563477
3-(4-fluorophenyl)-N-[3-fluoro-4-[[7-(3-pyrrolidin-1-ylpropanoyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C34H35F2N7O5
 1
1
IC50 = 290 nM
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CP0568457
N-[4-[[7-[2-(azetidin-1-yl)-2-oxoethyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C32H31F2N7O5
 1
1
IC50 = 370 nM
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CP0571003
N-[3-fluoro-4-[[7-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C34H36F2N8O5
 1
1
IC50 = 370 nM
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CP0368962
N-[4-[[7-(cyclobutanecarbonyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C32H30F2N6O5
 1
1
IC50 = 440 nM
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CP0565414
N-[3-fluoro-4-[(7-methyl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl)oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26F2N6O4
 1
1
IC50 = 570 nM
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CP0368965
N-[3-fluoro-4-[[7-(1-methylpiperidine-4-carbonyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C34H35F2N7O5
 1
1
IC50 = 630 nM
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CP0564987
N-[3-fluoro-4-[[6-(2-morpholin-4-ylacetyl)-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C32H31F2N7O6
 1
1
IC50 = 730 nM
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CP0565415
N-[3-fluoro-4-[(6-methyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl)oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26F2N6O4
 1
1
IC50 = 810 nM
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CP0539199
N-[3-fluoro-4-[[7-(2-morpholin-4-ylacetyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H33F2N7O6
 1
1
IC50 = 910 nM
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CP0568456
N-[3-fluoro-4-[(6-methyl-5,7-dihydropyrrolo[3,4-d]pyrimidin-4-yl)oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C27H24F2N6O4
 1
1
IC50 = 2600 nM
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CP0562062
1-cyclopropyl-N-[3-fluoro-4-[[7-[(1-methylpiperidin-4-yl)methyl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]oxy]phenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C34H35F2N7O4
 1
1
IC50 = 4110 nM
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Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01182 Tyrosine-protein kinase Mer Homo sapiens, Human