General Information of the Protein
Protein ID
PT01028
Protein Name
Ephrin type-B receptor 4
Secondarily
Protein Name
Hepatoma transmembrane kinase
Tyrosine-protein kinase TYRO11
Gene Name
EPHB4
Secondarily
Gene Name
HTK
MYK1
TYRO11
Sequence
MELRVLLCWASLAAALEETLLNTKLETADLKWVTFPQVDGQWEELSGLDEEQHSVRTYEVCDVQRAPGQAHWLRTGWVPRRGAVHVYATLRFTMLECLSLPRAGRSCKETFTVFYYESDADTATALTPAWMENPYIKVDTVAAEHLTRKRPGAEATGKVNVKTLRLGPLSKAGFYLAFQDQGACMALLSLHLFYKKCAQLTVNLTRFPETVPRELVVPVAGSCVVDAVPAPGPSPSLYCREDGQWAEQPVTGCSCAPGFEAAEGNTKCRACAQGTFKPLSGEGSCQPCPANSHSNTIGSAVCQCRVGYFRARTDPRGAPCTTPPSAPRSVVSRLNGSSLHLEWSAPLESGGREDLTYALRCRECRPGGSCAPCGGDLTFDPGPRDLVEPWVVVRGLRPDFTYTFEVTALNGVSSLATGPVPFEPVNVTTDREVPPAVSDIRVTRSSPSSLSLAWAVPRAPSGAVLDYEVKYHEKGAEGPSSVRFLKTSENRAELRGLKRGASYLVQVRARSEAGYGPFGQEHHSQTQLDESEGWREQLALIAGTAVVGVVLVLVVIVVAVLCLRKQSNGREAEYSDKHGQYLIGHGTKVYIDPFTYEDPNEAVREFAKEIDVSYVKIEEVIGAGEFGEVCRGRLKAPGKKESCVAIKTLKGGYTERQRREFLSEASIMGQFEHPNIIRLEGVVTNSMPVMILTEFMENGALDSFLRLNDGQFTVIQLVGMLRGIASGMRYLAEMSYVHRDLAARNILVNSNLVCKVSDFGLSRFLEENSSDPTYTSSLGGKIPIRWTAPEAIAFRKFTSASDAWSYGIVMWEVMSFGERPYWDMSNQDVINAIEQDYRLPPPPDCPTSLHQLMLDCWQKDRNARPRFPQVVSALDKMIRNPASLKIVARENGGASHPLLDQRQPHYSAFGSVGEWLRAIKMGRYEESFAAAGFGSFELVSQISAEDLLRIGVTLAGHQKKILASVQHMKSQAKPGTPGGTGGPAPQY
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Eph family
Function
Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Together with its cognate ligand/functional ligand EFNB2 it is involved in the regulation of cell adhesion and migration, and plays a central role in heart morphogenesis, angiogenesis and blood vessel remodeling and permeability. EPHB4-mediated forward signaling controls cellular repulsion and segregation from EFNB2-expressing cells.
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Uniprot ID
Primary ID:
P54760

Secondarily ID:
B5A970
B5A971
B5A972
Q7Z635
Q9BTA5
Q9BXP0
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Ensembl ID
ENSG00000196411
HGNC ID
HGNC:3395
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: CL000045 , A-375
Compound ID Compound Name Compound Formula
CP0672877
1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea
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C23H29FN6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019908
BDBM50242742
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C30H40ClN7O3S
 2
1 EC50 > 1000 nM
2 Kd = 750 nM
CP0233572
2-N-(2,6-dimorpholin-4-ylpyridin-4-yl)-4-N-(1H-indazol-4-yl)-4-N-methylpyrimidine-2,4-diamine
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C25H29N9O2
 1
1 IC50 = 0.9 nM
CP0554480
3-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)-5-(methylsulfonamido)benzenesulfonamide
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C18H17ClN6O6S2
 1
1 IC50 = 1 nM
CP0116958
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(1H-indazol-4-yl)-4-N-methylpyrimidine-2,4-diamine
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C26H30N8O2
 1
1 IC50 = 1.3 nM
CP0039399
8-(2-Methoxyphenyl)-1-methyl-7-(2'-methyl-5'-hydroxyphenyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
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C22H19N5O4
 2
1 IC50 = 1.6 nM
2 IC50 = 5 nM
CP0127575
4-N-(5-chloro-1,3-benzodioxol-4-yl)-2-N-(3,5-dimorpholin-4-ylphenyl)pyrimidine-2,4-diamine
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C25H27ClN6O4
 2
1 IC50 = 2 nM
2 IC50 = 4 nM
CP0352321
4-N-(5-chloro-1,3-benzodioxol-4-yl)-2-N-(3-methylsulfonyl-5-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
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C22H22ClN5O5S
 1
1 IC50 = 2 nM
CP0352322
N-[3-[[4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino]-5-morpholin-4-ylphenyl]methanesulfonamide
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C22H23ClN6O5S
 1
1 IC50 = 2 nM
CP0135850
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(3-methoxyphenyl)-4-N-methylpyrimidine-2,4-diamine
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C26H32N6O3
 1
1 IC50 = 2 nM
CP0135851
(3-(isopropyl(2-(3-(methylsulfonyl)-5-morpholinophenylamino)pyrimidin-4-yl)amino)-4-methylphenyl)methanol
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C26H33N5O4S
 1
1 IC50 = 2 nM
CP0207638
(2-chloro-5-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(methyl)amino)phenyl)methanol
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C26H31ClN6O3
 1
1 IC50 = 2 nM
CP0219293
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(methyl)amino)-5-methoxyphenyl)methanol
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C27H34N6O4
 1
1 IC50 = 2 nM
CP0253191
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(5-methoxypyridin-3-yl)-4-N-methylpyrimidine-2,4-diamine
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C25H31N7O3
 1
1 IC50 = 2 nM
CP0116959
2-N-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-N-(1H-indazol-4-yl)-4-N-methylpyrimidine-2,4-diamine
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C24H28N10O2
 1
1 IC50 = 2.6 nM
CP0207621
(4-methyl-3-(methyl(2-(3-(methylsulfonyl)-5-morpholinophenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C24H29N5O4S
 1
1 IC50 = 3 nM
CP0049382
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)methanol
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C27H34N6O3
 1
1 IC50 = 4 nM
CP0207620
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(ethyl)amino)-4-methylphenyl)methanol
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C28H36N6O3
 1
1 IC50 = 4 nM
CP0253757
(4-methyl-3-(methyl(2-(3-(4-methylpiperazin-1-yl)-5-morpholinophenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C28H37N7O2
 1
1 IC50 = 4 nM
CP0036684
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(isopropyl)amino)-4-methylphenyl)methanol
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C29H38N6O3
 1
1 IC50 = 5 nM
CP0171140
(3-((2-(3-methoxy-5-morpholinophenylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)methanol
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C24H29N5O3
 1
1 IC50 = 5 nM
CP0252942
(4-methyl-3-(methyl(2-(3-morpholino-5-(morpholinomethyl)phenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C28H36N6O3
 1
1 IC50 = 6 nM
CP0294196
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(6-methoxypyridin-2-yl)-4-N-methylpyrimidine-2,4-diamine
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C25H31N7O3
 1
1 IC50 = 6 nM
CP0300435
4-N-(3-chlorophenyl)-2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-methylpyrimidine-2,4-diamine
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C25H29ClN6O2
 1
1 IC50 = 6 nM
CP0271322
4-(3-(4-((5-(hydroxymethyl)-2-methylphenyl)(methyl)amino)pyrimidin-2-ylamino)-5-morpholinophenyl)piperazin-1-ol
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C27H35N7O3
 1
1 IC50 = 7 nM
CP0102613
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-methyl-4-N-(3-methylphenyl)pyrimidine-2,4-diamine
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C26H32N6O2
 1
1 IC50 = 8 nM
CP0135843
(4-methyl-3-(methyl(2-(3-morpholino-5-(tetrahydro-2H-pyran-4-yloxy)phenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C28H35N5O4
 1
1 IC50 = 8 nM
CP0300465
(3-((2-(3-(2-methoxyethoxy)-5-morpholinophenylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)methanol
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C26H33N5O4
 1
1 IC50 = 8 nM
CP0255598
(4-methyl-3-(methyl(2-(3-morpholino-5-(1,4-oxazepan-4-yl)phenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C28H36N6O3
 1
1 IC50 = 9 nM
CP0164812
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-methyl-4-N-(2-methylphenyl)pyrimidine-2,4-diamine
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C26H32N6O2
 1
1 IC50 = 10 nM
CP0222563
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(methyl)amino)phenyl)methanol
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C26H32N6O3
 1
1 IC50 = 10 nM
CP0253439
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(5-methoxy-2-methylphenyl)-4-N-methylpyrimidine-2,4-diamine
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C27H34N6O3
 1
1 IC50 = 10 nM
CP0313104
(4-methyl-3-(methyl(2-(3-morpholino-5-(piperidin-1-yl)phenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C28H36N6O2
 1
1 IC50 = 10 nM
CP0315162
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(1H-indazol-4-yl)pyrimidine-2,4-diamine
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C25H28N8O2
 1
1 IC50 = 11 nM
CP0197707
N-[3-[[4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino]-5-methylsulfonylphenyl]methanesulfonamide
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C19H18ClN5O6S2
 1
1 IC50 = 12 nM
CP0252926
(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(2-methoxyethyl)amino)-4-methylphenyl)methanol
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C29H38N6O4
 1
1 IC50 = 12 nM
CP0336576
3-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)-5-morpholinobenzamide
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C22H21ClN6O4
 1
1 IC50 = 13 nM
CP0256544
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(4-methoxypyridin-2-yl)-4-N-methylpyrimidine-2,4-diamine
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C25H31N7O3
 1
1 IC50 = 13 nM
CP0252925
(3-((2-(2,6-dimorpholinopyridin-4-ylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)methanol
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C26H33N7O3
 1
1 IC50 = 14 nM
CP0511559
N-[3-[[4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino]-5-(methanesulfonamido)phenyl]methanesulfonamide
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C19H19ClN6O6S2
 1
1 IC50 = 15 nM
CP0315192
(3-((2-(2,6-dimorpholinopyrimidin-4-ylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)methanol
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C25H32N8O3
 1
1 IC50 = 15 nM
CP0271323
(4-methyl-3-(methyl(2-(3-morpholino-5-(pyrrolidin-1-yl)phenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C27H34N6O2
 1
1 IC50 = 16 nM
CP0256543
(3-(4-((5-(hydroxymethyl)-2-methylphenyl)(methyl)amino)pyrimidin-2-ylamino)-5-morpholinophenyl)(morpholino)methanone
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C28H34N6O4
 1
1 IC50 = 17 nM
CP0292022
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-methyl-4-N-phenylpyrimidine-2,4-diamine
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C25H30N6O2
 1
1 IC50 = 17 nM
CP0135844
4-N-(2,5-dimethylphenyl)-2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-methylpyrimidine-2,4-diamine
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C27H34N6O2
 1
1 IC50 = 19 nM
CP0020367
3-(4-amino-3-(3-chloro-4-fluorophenyl)thieno[3,2-c]pyridin-7-yl)benzenesulfonamide
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C19H13ClFN3O2S2
 1
1 IC50 = 21 nM
CP0315164
(3-(4-((1H-indazol-4-yl)(methyl)amino)pyrimidin-2-ylamino)phenyl)methanol
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C19H18N6O
 1
1 IC50 = 21 nM
CP0206903
3-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)-5-(methylsulfonyl)benzamide
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C19H16ClN5O5S
 1
1 IC50 = 23 nM
CP0091881
2,4-Pyrimidine derivative, 28
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C18H15ClN4O4S
 2
1 IC50 = 25 nM
2 IC50 = 90 nM
CP0258762
3-(4-((1H-indazol-4-yl)(methyl)amino)pyrimidin-2-ylamino)-N,N-dimethylbenzamide
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C21H21N7O
 1
1 IC50 = 29 nM
CP0116956
4-N-(1,3-benzodioxol-4-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C18H16N4O4S
 1
1 IC50 = 34 nM
CP0218553
1-(3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl)(methyl)amino)-4-methylphenyl)ethanol
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C28H36N6O3
 1
1 IC50 = 35 nM
CP0225226
4-N-(5-chloro-1,3-benzodioxol-4-yl)-4-N-methyl-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C19H17ClN4O4S
 1
1 IC50 = 36 nM
CP0317073
4-N-(1H-indazol-4-yl)-4-N-methyl-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C19H18N6O2S
 1
1 IC50 = 36 nM
CP0185785
2,4-Pyrimidine derivative, 25
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C17H14ClN5O4S
 1
1 IC50 = 40 nM
CP0511413
2-(3-(4-amino-3-(3-chloro-4-fluorophenyl)thieno[3,2-c]pyridin-7-yl)phenyl)acetamide
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C21H15ClFN3OS
 1
1 IC50 = 44 nM
CP0059212
3-(3-chloro-4-fluorophenyl)-7-(pyridin-3-yl)thieno[3,2-c]pyridin-4-amine
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C18H11ClFN3S
 1
1 IC50 = 51 nM
CP0317074
4-N-(3-chloro-2H-indazol-4-yl)-2-N-(3,5-dimorpholin-4-ylphenyl)pyrimidine-2,4-diamine
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C25H27ClN8O2
 1
1 IC50 = 55 nM
CP0274585
3-(3-chloro-4-fluorophenyl)-7-(3-(methylsulfonyl)phenyl)thieno[3,2-c]pyridin-4-amine
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C20H14ClFN2O2S2
 1
1 IC50 = 59 nM
CP0258760
4-N-(1H-indazol-4-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C18H16N6O2S
 1
1 IC50 = 61 nM
CP0258763
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(3-methyl-2H-indazol-4-yl)pyrimidine-2,4-diamine
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C26H30N8O2
 1
1 IC50 = 67 nM
CP0197708
5-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)isophthalamide
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C19H15ClN6O4
 1
1 IC50 = 77 nM
CP0342841
N-[3-[[4-(1H-indazol-4-ylamino)pyrimidin-2-yl]amino]phenyl]methanesulfonamide
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C18H17N7O2S
 1
1 IC50 = 84 nM
CP0116957
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(1H-indazol-7-yl)pyrimidine-2,4-diamine
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C25H28N8O2
 1
1 IC50 = 89 nM
CP0258761
2-((5-chlorobenzo[d][1,3]dioxol-4-yl)(2-(3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)amino)acetonitrile
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C20H16ClN5O4S
 1
1 IC50 = 95 nM
CP0554479
2-N-[3,5-bis(methylsulfonyl)phenyl]-4-N-(5-chloro-1,3-benzodioxol-4-yl)pyrimidine-2,4-diamine
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C19H17ClN4O6S2
 1
1 IC50 = 114 nM
CP0105791
4-N-(2H-benzotriazol-4-yl)-2-N-(3,5-dimorpholin-4-ylphenyl)pyrimidine-2,4-diamine
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C24H27N9O2
 1
1 IC50 = 115 nM
CP0369740
2-N-(3,5-dimorpholin-4-ylphenyl)-4-N-(1H-indol-4-yl)pyrimidine-2,4-diamine
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C26H29N7O2
 1
1 IC50 = 117 nM
CP0127580
2-((5-chlorobenzo[d][1,3]dioxol-4-yl)(2-(3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)amino)ethanol
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C20H19ClN4O5S
 1
1 IC50 = 121 nM
CP0046280
1-amino-5-(5-hydroxy-2-methylphenyl)-7,8,9,10-tetrahydropyrimido[4,5-c]isoquinolin-6-one
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C18H18N4O2
 2
1 IC50 = 160 nM
2 IC50 = 300 nM
CP0315163
(3-(4-(1H-indazol-4-ylamino)pyrimidin-2-ylamino)phenyl)methanol
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C18H16N6O
 1
1 IC50 = 204 nM
CP0127578
4-N-(1-benzofuran-7-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C19H16N4O3S
 1
1 IC50 = 205 nM
CP0317733
4-N-(1,3-benzoxazol-7-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C18H15N5O3S
 1
1 IC50 = 219 nM
CP0090272
3-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)benzamide
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C18H14ClN5O3
 1
1 IC50 = 220 nM
CP0233571
3-(4-(1H-indazol-4-ylamino)pyrimidin-2-ylamino)-N,N-dimethylbenzamide
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C20H19N7O
 1
1 IC50 = 246 nM
CP0342840
4-N-(5-chloro-1,3-benzodioxol-4-yl)-4-N-(2-methoxyethyl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C21H21ClN4O5S
 1
1 IC50 = 246 nM
CP0369739
4-N-(6-chloro-1-benzofuran-7-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C19H15ClN4O3S
 1
1 IC50 = 300 nM
CP0344908
3-(4-(5-chlorobenzo[d][1,3]dioxol-4-ylamino)pyrimidin-2-ylamino)-5-(methylsulfonamido)benzamide
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C19H17ClN6O5S
 1
1 IC50 = 370 nM
CP0342842
2-N-(4,6-dimorpholin-4-ylpyrimidin-2-yl)-4-N-(1H-indazol-4-yl)-4-N-methylpyrimidine-2,4-diamine
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C24H28N10O2
 1
1 IC50 = 432 nM
CP0317072
4-N-(1,3-benzoxazol-4-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C18H15N5O3S
 1
1 IC50 = 549 nM
CP0086942
N-[3-[[4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino]phenyl]methanesulfonamide
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C18H16ClN5O4S
 1
1 IC50 = 794 nM
CP0127579
4-N-(2,3-dihydro-1-benzofuran-7-yl)-2-N-(3-methylsulfonylphenyl)pyrimidine-2,4-diamine
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C19H18N4O3S
 1
1 IC50 = 1160 nM
CP0140813
6-butyl-4-methyl-7-phenylpurino[7,8-a]imidazole-1,3-dione
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C18H19N5O2
 2
1 IC50 = 1500 nM
2 IC50 = 8300 nM
CP0302715
8-(2-methoxyphenyl)-1-methyl-7-phenyl-1H-imidazo[1,2-f]purine-2,4(3H,8H)-dione
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C21H17N5O3
 2
1 IC50 = 3300 nM
2 IC50 = 4350 nM
Clinical Information about the Protein
Target 1 ( Ephrin type-B receptor 4 (EPHB4) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Non-small-cell lung cancer [ICD-11: 2C25.Y]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 KD019 Phase 2
Non-small-cell lung cancer