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Compile Data Set for Download or QSAR

Found 1008 hits Enz. Inhib. hit(s) with Target = 'Tie-2' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Tie-2


(Homo sapiens (human))
BDBM50355491
PNG
(CHEMBL1835870)
Show SMILES Nc1nc(Nc2ccc(cc2)[C@H]2CC[C@@H](CC2)N2CCOCC2)nn1-c1ccccn1
Show InChI InChI=1S/C23H29N7O/c24-22-27-23(28-30(22)21-3-1-2-12-25-21)26-19-8-4-17(5-9-19)18-6-10-20(11-7-18)29-13-15-31-16-14-29/h1-5,8-9,12,18,20H,6-7,10-11,13-16H2,(H3,24,26,27,28)/t18-,20-
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200n/an/an/an/an/an/an/an/a



University of Kentucky

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50421257
PNG
(CHEMBL2087875)
Show SMILES C(CN1CCCC1)Oc1ccc(cc1)-c1[nH]c2ncnc(NCC3SCCS3)c2c1-c1ccccc1
Show InChI InChI=1S/C28H31N5OS2/c1-2-6-20(7-3-1)24-25-27(29-18-23-35-16-17-36-23)30-19-31-28(25)32-26(24)21-8-10-22(11-9-21)34-15-14-33-12-4-5-13-33/h1-3,6-11,19,23H,4-5,12-18H2,(H2,29,30,31,32)
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200n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of TIE2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50341519
PNG
((S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl...)
Show SMILES CNc1cncc(n1)-c1c[nH]c(=O)c(NC(=O)c2ccc(cc2)N2CCC[C@H]2CN2CCCC2)c1
Show InChI InChI=1S/C26H31N7O2/c1-27-24-16-28-15-23(30-24)19-13-22(26(35)29-14-19)31-25(34)18-6-8-20(9-7-18)33-12-4-5-21(33)17-32-10-2-3-11-32/h6-9,13-16,21H,2-5,10-12,17H2,1H3,(H,27,30)(H,29,35)(H,31,34)/t21-/m0/s1
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>1.00E+3n/an/an/an/an/an/an/an/a



Vertex Pharmaceuticals (Europe) Ltd.

Curated by ChEMBL


Assay Description
Inhibition of TIE2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50245852
PNG
(CHEMBL458333 | N3-(2,6-dimethylphenyl)-1-(3-methox...)
Show SMILES COC(C)(C)CCn1nc(Nc2c(C)cccc2C)c2cnc(Nc3ccc(OCCN4CCCC4)cc3)nc12
Show InChI InChI=1S/C31H41N7O2/c1-22-9-8-10-23(2)27(22)34-28-26-21-32-30(35-29(26)38(36-28)18-15-31(3,4)39-5)33-24-11-13-25(14-12-24)40-20-19-37-16-6-7-17-37/h8-14,21H,6-7,15-20H2,1-5H3,(H,34,36)(H,32,33,35)
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1.16E+3n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50245853
PNG
(CHEMBL502156 | N3-(2,6-dimethylphenyl)-N6-(3-fluor...)
Show SMILES COC(C)(C)CCn1nc(Nc2c(C)cccc2C)c2cnc(Nc3ccc(OCCN4CCCC4)c(F)c3)nc12
Show InChI InChI=1S/C31H40FN7O2/c1-21-9-8-10-22(2)27(21)35-28-24-20-33-30(36-29(24)39(37-28)16-13-31(3,4)40-5)34-23-11-12-26(25(32)19-23)41-18-17-38-14-6-7-15-38/h8-12,19-20H,6-7,13-18H2,1-5H3,(H,35,37)(H,33,34,36)
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>2.50E+3n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Protein-tyrosine kinase Tie2


(Homo sapiens (human))
BDBM50237710
PNG
(4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifl...)
Show SMILES Cc1cn(cn1)-c1cc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37)
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3.60E+3n/an/an/an/an/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by PDSP Ki Database




Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Tie-2


(Homo sapiens (human))
BDBM50245904
PNG
(CHEMBL459044 | N-(2,6-dimethylphenyl)-4-(2-ethoxyp...)
Show SMILES CCOc1ccccc1Oc1nc(Nc2ccc(cc2)N2CCNCC2)ncc1C(=O)Nc1c(C)cccc1C
Show InChI InChI=1S/C31H34N6O3/c1-4-39-26-10-5-6-11-27(26)40-30-25(29(38)35-28-21(2)8-7-9-22(28)3)20-33-31(36-30)34-23-12-14-24(15-13-23)37-18-16-32-17-19-37/h5-15,20,32H,4,16-19H2,1-3H3,(H,35,38)(H,33,34,36)
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>8.30E+3n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50297455
PNG
(1-((6-fluoro-4H-benzo[d][1,3]dioxin-8-yl)methyl)-3...)
Show SMILES Cc1ccc2C(N=O)C(=O)N(Cc3cc(F)cc4COCOc34)c2c1
Show InChI InChI=1S/C18H15FN2O4/c1-10-2-3-14-15(4-10)21(18(22)16(14)20-23)7-11-5-13(19)6-12-8-24-9-25-17(11)12/h2-6,16H,7-9H2,1H3
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>1.00E+4n/an/an/an/an/an/an/an/a



Vertex Pharmaceuticals Inc

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Protein-tyrosine kinase Tie2


(Homo sapiens (human))
BDBM13530
PNG
(4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[...)
Show SMILES CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Show InChI InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
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>1.00E+4n/an/an/an/an/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by PDSP Ki Database




Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Tie-2


(Homo sapiens (human))
BDBM50331612
PNG
(CHEMBL1290072 | N-(4-methoxybenzyl)benzofuro[2,3-b...)
Show SMILES COc1ccc(CNc2ccnc3oc4ccccc4c23)cc1
Show InChI InChI=1S/C19H16N2O2/c1-22-14-8-6-13(7-9-14)12-21-16-10-11-20-19-18(16)15-4-2-3-5-17(15)23-19/h2-11H,12H2,1H3,(H,20,21)
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>1.00E+6n/an/an/an/an/an/an/an/a



Martin Luther University Halle-Wittenberg

Curated by ChEMBL


Assay Description
Inhibition of human TIE2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50395892
PNG
(CHEMBL2163772)
Show SMILES Oc1ccc2oc3ncc(O)c(-c4ccccc4)c3c2c1
Show InChI InChI=1S/C17H11NO3/c19-11-6-7-14-12(8-11)16-15(10-4-2-1-3-5-10)13(20)9-18-17(16)21-14/h1-9,19-20H
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>1.00E+6n/an/an/an/an/an/an/an/a



Martin-Luther University Halle-Wittenberg

Curated by ChEMBL


Assay Description
Inhibition of TIE2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50266148
PNG
(CHEMBL465793 | N-(4-(3-(2-(methylamino)pyrimidin-4...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1ccc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C27H21N7O/c1-28-26-30-16-14-21(31-26)19-9-6-15-29-25(19)35-24-13-12-20(17-7-2-3-8-18(17)24)32-27-33-22-10-4-5-11-23(22)34-27/h2-16H,1H3,(H,28,30,31)(H2,32,33,34)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14974
PNG
(CHEMBL221484 | N-(3-(3-(Dimethylamino)propyl)-5-(t...)
Show SMILES CN(C)CCCc1cc(NC(=O)c2ccc(C)c(Nc3ncccc3-c3ccncn3)c2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C29H29F3N6O/c1-19-8-9-21(16-26(19)37-27-24(7-4-11-34-27)25-10-12-33-18-35-25)28(39)36-23-15-20(6-5-13-38(2)3)14-22(17-23)29(30,31)32/h4,7-12,14-18H,5-6,13H2,1-3H3,(H,34,37)(H,36,39)
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n/an/a 1n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tie-2


(Homo sapiens (human))
BDBM14948
PNG
(4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyrid...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2/c1-15-8-9-16(22(34)32-18-6-3-5-17(14-18)25(26,27)28)13-21(15)35-23-19(7-4-11-30-23)20-10-12-31-24(29-2)33-20/h3-14H,1-2H3,(H,32,34)(H,29,31,33)
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n/an/a<1n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Tie-2


(Homo sapiens (human))
BDBM14949
PNG
(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
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n/an/a 1n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14948
PNG
(4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyrid...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2/c1-15-8-9-16(22(34)32-18-6-3-5-17(14-18)25(26,27)28)13-21(15)35-23-19(7-4-11-30-23)20-10-12-31-24(29-2)33-20/h3-14H,1-2H3,(H,32,34)(H,29,31,33)
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n/an/a 1n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Tie-2


(Homo sapiens (human))
BDBM50192705
PNG
(1-(2-fluoro-5-methylphenyl)-3-{19-methyl-14-oxo-3-...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3cc(C)ccc3F)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C31H29FN6O2/c1-4-11-38-25-10-6-17(34-31(40)35-24-12-16(2)5-8-22(24)32)13-19(25)27-20-14-33-30(39)28(20)26-18(29(27)38)7-9-23-21(26)15-37(3)36-23/h5-6,8,10,12-13,15H,4,7,9,11,14H2,1-3H3,(H,33,39)(H2,34,35,40)
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n/an/a 1n/an/an/an/an/an/a



Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50266148
PNG
(CHEMBL465793 | N-(4-(3-(2-(methylamino)pyrimidin-4...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1ccc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C27H21N7O/c1-28-26-30-16-14-21(31-26)19-9-6-15-29-25(19)35-24-13-12-20(17-7-2-3-8-18(17)24)32-27-33-22-10-4-5-11-23(22)34-27/h2-16H,1H3,(H,28,30,31)(H2,32,33,34)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50207856
PNG
(3-isopropyl-N-(4-methyl-3-(3-(2-(methylamino)pyrid...)
Show SMILES CNc1cc(ccn1)-c1cccnc1Oc1cc(NC(=O)c2cccc(c2)C(C)C)ccc1C
Show InChI InChI=1S/C28H28N4O2/c1-18(2)20-7-5-8-22(15-20)27(33)32-23-11-10-19(3)25(17-23)34-28-24(9-6-13-31-28)21-12-14-30-26(16-21)29-4/h5-18H,1-4H3,(H,29,30)(H,32,33)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 after 90 mins by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14974
PNG
(CHEMBL221484 | N-(3-(3-(Dimethylamino)propyl)-5-(t...)
Show SMILES CN(C)CCCc1cc(NC(=O)c2ccc(C)c(Nc3ncccc3-c3ccncn3)c2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C29H29F3N6O/c1-19-8-9-21(16-26(19)37-27-24(7-4-11-34-27)25-10-12-33-18-35-25)28(39)36-23-15-20(6-5-13-38(2)3)14-22(17-23)29(30,31)32/h4,7-12,14-18H,5-6,13H2,1-3H3,(H,34,37)(H,36,39)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 after 90 mins by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tie-2


(Homo sapiens (human))
BDBM50207855
PNG
(CHEMBL245744 | N-(3-isopropylphenyl)-4-methyl-3-(3...)
Show SMILES CNc1ncnc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cccc(c1)C(C)C
Show InChI InChI=1S/C26H26N6O2/c1-16(2)18-7-5-8-20(13-18)31-24(33)19-11-10-17(3)22(14-19)34-25-21(9-6-12-28-25)23-29-15-30-26(27-4)32-23/h5-16H,1-4H3,(H,31,33)(H,27,29,30,32)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 after 90 mins by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50207852
PNG
(3-isopropyl-N-(4-methyl-3-(3-(4-(methylamino)-1,3,...)
Show SMILES CNc1ncnc(n1)-c1cccnc1Oc1cc(NC(=O)c2cccc(c2)C(C)C)ccc1C
Show InChI InChI=1S/C26H26N6O2/c1-16(2)18-7-5-8-19(13-18)24(33)31-20-11-10-17(3)22(14-20)34-25-21(9-6-12-28-25)23-29-15-30-26(27-4)32-23/h5-16H,1-4H3,(H,31,33)(H,27,29,30,32)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 after 90 mins by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50375682
PNG
(CHEMBL270057)
Show SMILES COc1cc2nccc(Oc3ccc4N(CCOc4c3)C(=O)Nc3cccc(C)c3)c2cc1OC
Show InChI InChI=1S/C27H25N3O5/c1-17-5-4-6-18(13-17)29-27(31)30-11-12-34-24-14-19(7-8-22(24)30)35-23-9-10-28-21-16-26(33-3)25(32-2)15-20(21)23/h4-10,13-16H,11-12H2,1-3H3,(H,29,31)
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n/an/a 1n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50319571
PNG
(CHEMBL1084451 | N-(4-(3-(2-((1-ethylpiperidin-4-yl...)
Show SMILES CCN1CCC(CNc2nccc(n2)-c2cccnc2Oc2ccc(Nc3nc4ccccc4[nH]3)c3ccccc23)CC1
Show InChI InChI=1S/C34H34N8O/c1-2-42-20-16-23(17-21-42)22-37-33-36-19-15-28(38-33)26-10-7-18-35-32(26)43-31-14-13-27(24-8-3-4-9-25(24)31)39-34-40-29-11-5-6-12-30(29)41-34/h3-15,18-19,23H,2,16-17,20-22H2,1H3,(H,36,37,38)(H2,39,40,41)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM35317
PNG
(4-Methyl-3-(2-(methylamino)quinazolin-6-yl)-N-(3-(...)
Show SMILES CNc1ncc2cc(ccc2n1)-c1cc(ccc1C)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C24H19F3N4O/c1-14-6-7-16(22(32)30-19-5-3-4-18(12-19)24(25,26)27)11-20(14)15-8-9-21-17(10-15)13-29-23(28-2)31-21/h3-13H,1-2H3,(H,30,32)(H,28,29,31)
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n/an/a 1.80n/an/an/an/a7.523



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM5815
PNG
(3-{4-[4-amino-6-(4-methoxyphenyl)furo[2,3-d]pyrimi...)
Show SMILES COc1ccc(cc1)-c1oc2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)cc1
Show InChI InChI=1S/C27H19F4N5O3/c1-38-18-9-4-15(5-10-18)23-21(22-24(32)33-13-34-25(22)39-23)14-2-7-17(8-3-14)35-26(37)36-20-12-16(27(29,30)31)6-11-19(20)28/h2-13H,1H3,(H2,32,33,34)(H2,35,36,37)
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n/an/a 2n/an/an/an/a7.522



GlaxoSmithKline



Assay Description
The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14949
PNG
(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
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n/an/a 2n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14967
PNG
(3-(2-(3H-Imidazo[4,5-b]pyridin-6-yl)ethynyl)-4-met...)
Show SMILES Cc1ccc(cc1C#Cc1cnc2nc[nH]c2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H15F3N4O/c1-14-5-7-17(22(31)30-19-4-2-3-18(11-19)23(24,25)26)10-16(14)8-6-15-9-20-21(27-12-15)29-13-28-20/h2-5,7,9-13H,1H3,(H,30,31)(H,27,28,29)
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n/an/a 2n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14949
PNG
(2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-...)
Show SMILES Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C23H17F3N4O/c1-13-5-6-15(21(31)29-18-4-2-3-17(11-18)23(24,25)26)10-19(13)14-7-8-20-16(9-14)12-28-22(27)30-20/h2-12H,1H3,(H,29,31)(H2,27,28,30)
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Amgen



Assay Description
The assay involves the phosphorylation of a biotinylated substrate and the detection of this phosphorylation after the addition of a streptavidin-all...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50266221
PNG
(CHEMBL458023 | N-(3-methyl-4-(3-(2-(methylamino)py...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1c(C)cc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C28H23N7O/c1-17-16-24(35-28-33-22-11-5-6-12-23(22)34-28)18-8-3-4-9-19(18)25(17)36-26-20(10-7-14-30-26)21-13-15-31-27(29-2)32-21/h3-16H,1-2H3,(H,29,31,32)(H2,33,34,35)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50319572
PNG
(CHEMBL1084452 | N-(4-(3-(2-(2-(1-methylpyrrolidin-...)
Show SMILES CN1CCCC1CCNc1nccc(n1)-c1cccnc1Oc1ccc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C33H32N8O/c1-41-21-7-8-22(41)16-19-35-32-36-20-17-27(37-32)25-11-6-18-34-31(25)42-30-15-14-26(23-9-2-3-10-24(23)30)38-33-39-28-12-4-5-13-29(28)40-33/h2-6,9-15,17-18,20,22H,7-8,16,19,21H2,1H3,(H,35,36,37)(H2,38,39,40)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50236270
PNG
(1-(4-(4-amino-6-(4-methoxyphenyl)furo[2,3-d]pyrimi...)
Show SMILES COc1ccc(cc1)-c1oc2ncnc(N)c2c1-c1ccc(NC(=O)Nc2c(F)cccc2C(F)(F)F)cc1
Show InChI InChI=1S/C27H19F4N5O3/c1-38-17-11-7-15(8-12-17)23-20(21-24(32)33-13-34-25(21)39-23)14-5-9-16(10-6-14)35-26(37)36-22-18(27(29,30)31)3-2-4-19(22)28/h2-13H,1H3,(H2,32,33,34)(H2,35,36,37)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human recombinant TIE2 by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192708
PNG
(1-(2-fluorophenyl)-3-{19-methyl-14-oxo-3-propyl-3,...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3ccccc3F)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C30H27FN6O2/c1-3-12-37-24-11-8-16(33-30(39)34-23-7-5-4-6-21(23)31)13-18(24)26-19-14-32-29(38)27(19)25-17(28(26)37)9-10-22-20(25)15-36(2)35-22/h4-8,11,13,15H,3,9-10,12,14H2,1-2H3,(H,32,38)(H2,33,34,39)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192712
PNG
(1-methyl-3-{19-methyl-14-oxo-3-propyl-3,13,19,20-t...)
Show SMILES CCCn1c2ccc(NC(=O)N(C)c3ccccc3)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C31H30N6O2/c1-4-14-37-25-13-10-18(33-31(39)36(3)19-8-6-5-7-9-19)15-21(25)27-22-16-32-30(38)28(22)26-20(29(27)37)11-12-24-23(26)17-35(2)34-24/h5-10,13,15,17H,4,11-12,14,16H2,1-3H3,(H,32,38)(H,33,39)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192714
PNG
(1-(4-methoxyphenyl)-3-{19-methyl-14-oxo-3-propyl-3...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3ccc(OC)cc3)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C31H30N6O3/c1-4-13-37-25-12-7-18(34-31(39)33-17-5-8-19(40-3)9-6-17)14-21(25)27-22-15-32-30(38)28(22)26-20(29(27)37)10-11-24-23(26)16-36(2)35-24/h5-9,12,14,16H,4,10-11,13,15H2,1-3H3,(H,32,38)(H2,33,34,39)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192709
PNG
(1-(3-fluorophenyl)-3-{19-methyl-14-oxo-3-propyl-3,...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3cccc(F)c3)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C30H27FN6O2/c1-3-11-37-24-10-7-18(34-30(39)33-17-6-4-5-16(31)12-17)13-20(24)26-21-14-32-29(38)27(21)25-19(28(26)37)8-9-23-22(25)15-36(2)35-23/h4-7,10,12-13,15H,3,8-9,11,14H2,1-2H3,(H,32,38)(H2,33,34,39)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192722
PNG
(1-(4-fluorophenyl)-3-{19-methyl-14-oxo-3-propyl-3,...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3ccc(F)cc3)cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12
Show InChI InChI=1S/C30H27FN6O2/c1-3-12-37-24-11-8-18(34-30(39)33-17-6-4-16(31)5-7-17)13-20(24)26-21-14-32-29(38)27(21)25-19(28(26)37)9-10-23-22(25)15-36(2)35-23/h4-8,11,13,15H,3,9-10,12,14H2,1-2H3,(H,32,38)(H2,33,34,39)
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Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50266221
PNG
(CHEMBL458023 | N-(3-methyl-4-(3-(2-(methylamino)py...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1c(C)cc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C28H23N7O/c1-17-16-24(35-28-33-22-11-5-6-12-23(22)34-28)18-8-3-4-9-19(18)25(17)36-26-20(10-7-14-30-26)21-13-15-31-27(29-2)32-21/h3-16H,1-2H3,(H,29,31,32)(H2,33,34,35)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50207850
PNG
(3-isopropyl-N-(4-methyl-3-(3-(2-(methylamino)pyrim...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1cc(NC(=O)c2cccc(c2)C(C)C)ccc1C
Show InChI InChI=1S/C27H27N5O2/c1-17(2)19-7-5-8-20(15-19)25(33)31-21-11-10-18(3)24(16-21)34-26-22(9-6-13-29-26)23-12-14-30-27(28-4)32-23/h5-17H,1-4H3,(H,31,33)(H,28,30,32)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 after 90 mins by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50266221
PNG
(CHEMBL458023 | N-(3-methyl-4-(3-(2-(methylamino)py...)
Show SMILES CNc1nccc(n1)-c1cccnc1Oc1c(C)cc(Nc2nc3ccccc3[nH]2)c2ccccc12
Show InChI InChI=1S/C28H23N7O/c1-17-16-24(35-28-33-22-11-5-6-12-23(22)34-28)18-8-3-4-9-19(18)25(17)36-26-20(10-7-14-30-26)21-13-15-31-27(29-2)32-21/h3-16H,1-2H3,(H,29,31,32)(H2,33,34,35)
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n/an/a 2n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM5815
PNG
(3-{4-[4-amino-6-(4-methoxyphenyl)furo[2,3-d]pyrimi...)
Show SMILES COc1ccc(cc1)-c1oc2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)cc1
Show InChI InChI=1S/C27H19F4N5O3/c1-38-18-9-4-15(5-10-18)23-21(22-24(32)33-13-34-25(22)39-23)14-2-7-17(8-3-14)35-26(37)36-20-12-16(27(29,30)31)6-11-19(20)28/h2-13H,1H3,(H2,32,33,34)(H2,35,36,37)
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n/an/a 2n/an/an/an/an/an/a



Dalian University

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50345579
PNG
(5-((5-(4-((4-(2-hydroxyethyl)piperazin-1-yl)methyl...)
Show SMILES CNC(=O)c1ncc(C#Cc2cc(ccc2C)C(=O)Nc2ccc(CN3CCN(CCO)CC3)c(c2)C(F)(F)F)n1C
Show InChI InChI=1S/C30H33F3N6O3/c1-20-4-5-22(16-21(20)7-9-25-18-35-27(37(25)3)29(42)34-2)28(41)36-24-8-6-23(26(17-24)30(31,32)33)19-39-12-10-38(11-13-39)14-15-40/h4-6,8,16-18,40H,10-15,19H2,1-3H3,(H,34,42)(H,36,41)
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n/an/a 2.20n/an/an/an/an/an/a



ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human Tie2/TEK using poly[Glu:Tyr] by Hotspot assay


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM17806
PNG
(N-{6-[4-({[2-fluoro-5-(trifluoromethyl)phenyl]carb...)
Show SMILES CC(=O)Nc1nc2ccc(Oc3ccc(NC(=O)Nc4cc(ccc4F)C(F)(F)F)cc3)cc2[nH]1
Show InChI InChI=1S/C23H17F4N5O3/c1-12(33)28-21-30-18-9-7-16(11-20(18)31-21)35-15-5-3-14(4-6-15)29-22(34)32-19-10-13(23(25,26)27)2-8-17(19)24/h2-11H,1H3,(H2,29,32,34)(H2,28,30,31,33)
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n/an/a 2.60n/an/an/an/a7.422



GSK



Assay Description
The assay uses purified GST-Tie-2 or GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium cryptate...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM17805
PNG
(N-(6-{[6-({[2-fluoro-5-(trifluoromethyl)phenyl]car...)
Show SMILES CC(=O)Nc1nc2ccc(Oc3ccc(NC(=O)Nc4cc(ccc4F)C(F)(F)F)nc3)cc2[nH]1
Show InChI InChI=1S/C22H16F4N6O3/c1-11(33)28-20-29-16-6-3-13(9-18(16)30-20)35-14-4-7-19(27-10-14)32-21(34)31-17-8-12(22(24,25)26)2-5-15(17)23/h2-10H,1H3,(H2,27,31,32,34)(H2,28,29,30,33)
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n/an/a 2.90n/an/an/an/a7.422



GSK



Assay Description
The assay uses purified GST-Tie-2 or GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium cryptate...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM17823
PNG
(N-{6-[4-({[2-fluoro-5-(trifluoromethyl)phenyl]carb...)
Show SMILES COCCOCC(=O)Nc1nc2ccc(Oc3ccc(NC(=O)Nc4cc(ccc4F)C(F)(F)F)cc3)cc2[nH]1
Show InChI InChI=1S/C26H23F4N5O5/c1-38-10-11-39-14-23(36)35-24-32-20-9-7-18(13-22(20)33-24)40-17-5-3-16(4-6-17)31-25(37)34-21-12-15(26(28,29)30)2-8-19(21)27/h2-9,12-13H,10-11,14H2,1H3,(H2,31,34,37)(H2,32,33,35,36)
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n/an/a 3n/an/an/an/a7.422



GSK



Assay Description
The assay uses purified GST-Tie-2 or GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium cryptate...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192724
PNG
(3-{10-carboximidoyl-5-oxo-14-propyl-4,14-diazapent...)
Show SMILES CCCn1c2ccc(NC(=O)Nc3ccc(C)cc3)cc2c2c3CNC(=O)c3c3CC=C(Cc3c12)C=N
Show InChI InChI=1S/C30H29N5O2/c1-3-12-35-25-11-9-20(34-30(37)33-19-7-4-17(2)5-8-19)14-23(25)26-24-16-32-29(36)27(24)21-10-6-18(15-31)13-22(21)28(26)35/h4-9,11,14-15,31H,3,10,12-13,16H2,1-2H3,(H,32,36)(H2,33,34,37)
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n/an/a 3n/an/an/an/an/an/a



Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50318963
PNG
(CHEMBL1084061 | rac-5-methyl-9-propyl-12-(tetrahyd...)
Show SMILES CCCn1c2ccc(cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12)C1CCCCO1
Show InChI InChI=1S/C28H30N4O2/c1-3-11-32-22-10-7-16(23-6-4-5-12-34-23)13-18(22)25-19-14-29-28(33)26(19)24-17(27(25)32)8-9-21-20(24)15-31(2)30-21/h7,10,13,15,23H,3-6,8-9,11-12,14H2,1-2H3,(H,29,33)
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n/an/a 3n/an/an/an/an/an/a



Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human recombinant TIE-2 by time resolved fluorescence measurements


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM14966
PNG
(3-(2-(6-Aminopyridin-3-yl)ethynyl)-4-methyl-N-(3-(...)
Show SMILES Cc1ccc(cc1C#Cc1ccc(N)nc1)C(=O)Nc1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C22H16F3N3O/c1-14-5-8-17(11-16(14)9-6-15-7-10-20(26)27-13-15)21(29)28-19-4-2-3-18(12-19)22(23,24)25/h2-5,7-8,10-13H,1H3,(H2,26,27)(H,28,29)
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n/an/a 3n/an/an/an/a7.522



Amgen



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50192701
PNG
(1-(4-methoxyphenyl)-3-[19-methyl-3-(2-methylpropyl...)
Show SMILES COc1ccc(NC(=O)Nc2ccc3n(CC(C)C)c4c5CCc6nn(C)cc6-c5c5C(=O)NCc5c4c3c2)cc1
Show InChI InChI=1S/C32H32N6O3/c1-17(2)15-38-26-12-7-19(35-32(40)34-18-5-8-20(41-4)9-6-18)13-22(26)28-23-14-33-31(39)29(23)27-21(30(28)38)10-11-25-24(27)16-37(3)36-25/h5-9,12-13,16-17H,10-11,14-15H2,1-4H3,(H,33,39)(H2,34,35,40)
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n/an/a 3n/an/an/an/an/an/a



Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Tie2


Citation and Details
More data for this
Ligand-Target Pair
Tie-2


(Homo sapiens (human))
BDBM50318959
PNG
(CHEMBL1084337 | rac-9-isobutyl-5-methyl-12-(tetrah...)
Show SMILES CC(C)Cn1c2ccc(cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12)C1CCCCO1
Show InChI InChI=1S/C29H32N4O2/c1-16(2)14-33-23-10-7-17(24-6-4-5-11-35-24)12-19(23)26-20-13-30-29(34)27(20)25-18(28(26)33)8-9-22-21(25)15-32(3)31-22/h7,10,12,15-16,24H,4-6,8-9,11,13-14H2,1-3H3,(H,30,34)
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n/an/a 3n/an/an/an/an/an/a



Cephalon, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human recombinant TIE-2 by time resolved fluorescence measurements


Citation and Details
More data for this
Ligand-Target Pair
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