General Information of the Protein
Protein ID
PT01182
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
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQPALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVPNIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKINNEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNEQPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSILISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVSCMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGYRISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFIPAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTEEDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMSSQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPDSIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGERLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Axl family
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 (PubMed:32640697). 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:
Q12866

Secondarily ID:
Q9HBB4
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Ensembl ID
ENSG00000153208
HGNC ID
HGNC:7027
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
CP0317631
N-[2,5-difluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C36H39F3N8O5
 1
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
CP0563520
1-cyclopentyl-N-[3-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C35H36F2N6O5
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0557698
N-[2-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H34F2N6O5
 1
1
IC50 = 8.1 nM
   TI
   LI
   LO
   TS
CP0564219
3-(4-fluorophenyl)-N-[4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H35FN6O5
 1
1
IC50 = 9.8 nM
   TI
   LI
   LO
   TS
CP0553502
N-[2,5-difluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-2,5-dioxo-1-phenyl-7,8-dihydro-6H-quinoline-3-carboxamide
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C38H39F2N7O5
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0557697
N-[4-[6-(cyclopropanecarbonylamino)pyrimidin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H25FN6O5
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0553501
1-cyclopentyl-3-(4-fluorophenyl)-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C37H42FN9O5
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0554516
1-cyclopropyl-N-[3-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C33H32F2N6O5
 1
1
IC50 = 44 nM
   TI
   LI
   LO
   TS
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
   TI
   LI
   LO
   TS
CP0543363
N-[4-[6-(azetidine-1-carbonylamino)pyrimidin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26FN7O5
 1
1
IC50 = 66 nM
   TI
   LI
   LO
   TS
CP0563666
N-[4-[2-[[2-(dimethylamino)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C29H29FN6O5
 1
1
IC50 = 68 nM
   TI
   LI
   LO
   TS
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0554517
3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-yl-N-[4-[6-(pyrrolidine-1-carbonylamino)pyrimidin-4-yl]oxyphenyl]pyrimidine-5-carboxamide
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C29H28FN7O5
 1
1
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0563667
3-(4-fluorophenyl)-N-[4-[6-[(3-hydroxyazetidine-1-carbonyl)amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26FN7O6
 1
1
IC50 = 113 nM
   TI
   LI
   LO
   TS
CP0317628
3-(4-fluorophenyl)-N-[4-[6-[[3-(methylamino)azetidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C29H29FN8O5
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0317629
3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-yl-N-[4-[6-[(3-pyrrolidin-1-ylazetidine-1-carbonyl)amino]pyrimidin-4-yl]oxyphenyl]pyrimidine-5-carboxamide
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C32H33FN8O5
 1
1
IC50 = 157 nM
   TI
   LI
   LO
   TS
CP0566934
1-cyclopropyl-3-(4-fluorophenyl)-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C35H38FN9O5
 1
1
IC50 = 304 nM
   TI
   LI
   LO
   TS
CP0570986
3-(4-fluorophenyl)-1-methyl-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C33H36FN9O5
 1
1
IC50 = 321 nM
   TI
   LI
   LO
   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
 1
1
IC50 = 4700 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 1
1
IC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
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CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
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CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 > 8700 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0051296
CHEMBL3326006
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C28H40N6O
 1
1 IC50 = 0.74 nM
CP0140081
(6S)-6-amino-22-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,8,17,19,25-pentazatricyclo[16.5.2.021,24]pentacosa-18,20,22,24-tetraen-7-one
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C32H48N8O
 1
1 IC50 = 0.8 nM
CP0329747
(2,6-dimethylpyridin-4- yl)(4-(7-((1R,4S)-4- hydroxycyclohexyl)-2- (((S)-pentan-2-yl)amino)- 7H-pyrrolo[2,3- d]pyrimidin-5-yl)piperidin- 1-yl)methanone
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C30H42N6O2
 2
1 IC50 = 0.9 nM
2 Ki = 0.19 nM
CP0200346
CHEMBL3092807
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C24H36N6O2
 1
1 IC50 = 1.7 nM
CP0176167
18-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,13,15,21-tetrazatricyclo[12.5.2.017,20]henicosa-14,16,18,20-tetraen-5-ol
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C29H42N6O
 1
1 IC50 = 1.8 nM
CP0198243
(6S)-6-amino-20-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,8,15,17,23-pentazatricyclo[14.5.2.019,22]tricosa-16,18,20,22-tetraen-7-one
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C30H44N8O
 1
1 IC50 = 2.2 nM
CP0115610
CHEMBL4283353
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C30H44N6O
 2
1 IC50 = 2.4 nM
2 Ki = 0.43 nM
CP0046963
20-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,15,17,23-tetrazatricyclo[14.5.2.019,22]tricosa-16,18,20,22-tetraen-6-ol
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C31H46N6O
 1
1 IC50 = 2.6 nM
CP0126327
CHEMBL2036808
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C22H29FN6
 2
1 IC50 = 2.9 nM
2 Ki = 4.3 nM
CP0085838
19-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C30H44N6O
 1
1 IC50 = 3 nM
CP0326622
20-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,15,17,23-tetrazatricyclo[14.5.2.019,22]tricosa-16,18,20,22-tetraen-7-ol
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C31H46N6O
 1
1 IC50 = 3.1 nM
CP0140011
(5S)-5-amino-17-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,7,12,14,20-pentazatricyclo[11.5.2.016,19]icosa-13,15,17,19-tetraen-6-one
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C27H38N8O
 1
1 IC50 = 3.9 nM
CP0046964
16-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,11,13,19-tetrazatricyclo[10.5.2.015,18]nonadeca-12,14,16,18-tetraen-5-ol
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C27H38N6O
 1
1 IC50 = 4.1 nM
CP0060304
18-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,13,15,21-tetrazatricyclo[12.5.2.017,20]henicosa-14,16,18,20-tetraen-7-ol
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C29H42N6O
 1
1 IC50 = 4.1 nM
CP0557697
N-[4-[6-(cyclopropanecarbonylamino)pyrimidin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H25FN6O5
 1
1 IC50 < 4.1 nM
CP0134339
CHEMBL3093756
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C25H33N7O2
 1
1 IC50 = 4.3 nM
CP0176174
21-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,16,18,24-tetrazatricyclo[15.5.2.020,23]tetracosa-17,19,21,23-tetraen-7-ol
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C32H48N6O
 1
1 IC50 = 4.9 nM
CP0198240
19-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-7-ol
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C30H44N6O
 1
1 IC50 = 5 nM
CP0140241
17-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,12,14,20-tetrazatricyclo[11.5.2.016,19]icosa-13,15,17,19-tetraen-5-ol
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C28H40N6O
 1
1 IC50 = 5.6 nM
CP0557698
N-[2-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H34F2N6O5
 1
1 IC50 = 6.8 nM
CP0558278
17-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,12,14,20-tetrazatricyclo[11.5.2.016,19]icosa-13,15,17,19-tetraen-6-ol
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C28H40N6O
 1
1 IC50 = 8 nM
CP0564219
3-(4-fluorophenyl)-N-[4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C33H35FN6O5
 1
1 IC50 = 8 nM
CP0198242
[4-(6-hydroxy-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-19-yl)phenyl]-morpholin-4-ylmethanone
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C29H39N5O3
 1
1 IC50 = 8.1 nM
CP0180230
(6S)-6-amino-18-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,8,13,15,21-pentazatricyclo[12.5.2.017,20]henicosa-14,16,18,20-tetraen-7-one
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C28H40N8O
 1
1 IC50 = 8.9 nM
CP0046837
19-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-5-ol
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C30H44N6O
 1
1 IC50 = 9.6 nM
CP0060303
19-(4-morpholin-4-ylsulfonylphenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C28H39N5O4S
 1
1 IC50 = 11 nM
CP0553501
1-cyclopentyl-3-(4-fluorophenyl)-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C37H42FN9O5
 1
1 IC50 = 11 nM
CP0046996
19-pyridin-3-yl-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C23H31N5O
 1
1 IC50 = 13 nM
CP0543363
N-[4-[6-(azetidine-1-carbonylamino)pyrimidin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26FN7O5
 1
1 IC50 = 13 nM
CP0094327
19-[4-(morpholin-4-ylmethyl)phenyl]-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C29H41N5O2
 1
1 IC50 = 16 nM
CP0563520
1-cyclopentyl-N-[3-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C35H36F2N6O5
 1
1 IC50 = 16 nM
CP0140010
(5S)-5-amino-19-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,7,14,16,22-pentazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-one
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C29H42N8O
 1
1 IC50 = 17 nM
CP0563666
N-[4-[2-[[2-(dimethylamino)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C29H29FN6O5
 1
1 IC50 = 18 nM
CP0554516
1-cyclopropyl-N-[3-fluoro-4-[2-[[2-(1-methylpiperidin-4-yl)acetyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxopyrimidine-5-carboxamide
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C33H32F2N6O5
 1
1 IC50 = 22 nM
CP0553502
N-[2,5-difluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-2,5-dioxo-1-phenyl-7,8-dihydro-6H-quinoline-3-carboxamide
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C38H39F2N7O5
 1
1 IC50 = 25 nM
CP0563667
3-(4-fluorophenyl)-N-[4-[6-[(3-hydroxyazetidine-1-carbonyl)amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C28H26FN7O6
 1
1 IC50 = 25 nM
CP0554517
3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-yl-N-[4-[6-(pyrrolidine-1-carbonylamino)pyrimidin-4-yl]oxyphenyl]pyrimidine-5-carboxamide
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C29H28FN7O5
 1
1 IC50 = 28 nM
CP0140014
N-[4-(6-hydroxy-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-19-yl)phenyl]morpholine-4-carboxamide
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C29H40N6O3
 1
1 IC50 = 30 nM
CP0198241
(5S)-5-amino-21-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1,7,16,18,24-pentazatricyclo[15.5.2.020,23]tetracosa-17,19,21,23-tetraen-6-one
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C31H46N8O
 1
1 IC50 = 30 nM
CP0046834
19-(4-morpholin-4-ylphenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C28H39N5O2
 1
1 IC50 = 32 nM
CP0317631
N-[2,5-difluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C36H39F3N8O5
 1
1 IC50 = 36 nM
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 = 38 nM
CP0046839
19-pyridin-2-yl-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C23H31N5O
 1
1 IC50 = 54 nM
CP0317628
3-(4-fluorophenyl)-N-[4-[6-[[3-(methylamino)azetidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide
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C29H29FN8O5
 1
1 IC50 = 64 nM
CP0317629
3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-yl-N-[4-[6-[(3-pyrrolidin-1-ylazetidine-1-carbonyl)amino]pyrimidin-4-yl]oxyphenyl]pyrimidine-5-carboxamide
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C32H33FN8O5
 1
1 IC50 = 79 nM
CP0140008
19-pyridin-4-yl-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C23H31N5O
 1
1 IC50 = 80 nM
CP0140013
19-(4-methoxyphenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C25H34N4O2
 1
1 IC50 = 86 nM
CP0180227
19-(oxan-4-yl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C23H36N4O2
 1
1 IC50 = 94 nM
CP0094329
19-phenyl-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C24H32N4O
 1
1 IC50 = 140 nM
CP0046998
19-(4-fluorophenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C24H31FN4O
 1
1 IC50 = 150 nM
CP0570986
3-(4-fluorophenyl)-1-methyl-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C33H36FN9O5
 1
1 IC50 = 157 nM
CP0176118
19-(3-methoxyphenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C25H34N4O2
 1
1 IC50 = 160 nM
CP0060311
19-(2-methoxyphenyl)-1,14,16,22-tetrazatricyclo[13.5.2.018,21]docosa-15,17,19,21-tetraen-6-ol
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C25H34N4O2
 1
1 IC50 = 170 nM
CP0566934
1-cyclopropyl-3-(4-fluorophenyl)-N-[4-[6-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyrimidin-4-yl]oxyphenyl]-2,4-dioxopyrimidine-5-carboxamide
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C35H38FN9O5
 1
1 IC50 = 234 nM
CP0018808
4-(cyclopentylamino)-2-[(2,5-dichlorophenyl)methylamino]-N-[3-(2-oxo-1,3-oxazolidin-3-yl)propyl]pyrimidine-5-carboxamide
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C23H28Cl2N6O3
 2
1 IC50 = 775 nM
2 Kd = 570 nM
Clinical Information about the Protein
Target 1 ( Tyrosine-protein kinase Mer (MERTK) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Alzheimer disease [ICD-11: 8A20]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 MK-2461 Phase 1/2
Alzheimer disease
2 RXDX-106 Phase 1
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT07205 Tyrosine-protein kinase Mer Mus musculus, Mouse