Target Poor or Non Binder(s) Information

Target General Information

Target ID

T92144

Target Info

Target Name

Angiopoietin 1 receptor (TEK)

Synonyms

hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b

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Target Type

Clinical trial Target

Gene Name

TEK

Biochemical Class

Kinase

UniProt ID

Q02763

Poor Binders of This Target (in total, 29 binders)

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Compound Name

Niclosamide

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Approved

Compound Info

Synonyms

niclosamide; 50-65-7; Niclocide; 5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide; Tredemine; Bayluscid; Phenasal; Yomesan; Fenasal; Dichlosale; Helmiantin; Sagimid; Iomezan; Devermine; Atenase; Vermitid; Radeverm; Mansonil; Iomesan; Devermin; Cestocid; Sulqui; Lintex; Nasemo; Mato; Fedal-Telmin; Bayer 73; Radewerm; Zestocarp; Bayer 2353; 2',5-Dichloro-4'-nitrosalicylanilide; Chemagro 2353; BAY 2353; Benzamide, 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-; 5-Chloro-2'-chloro-4'-nitrosalicylanilide; nicolsamide; HL 2447; Niclosamidum [I

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Activity

IC50 = 67800 nM

[1]

Compound Name

A-770041

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Investigative

Compound Info

Synonyms

A-770041; 869748-10-7; UNII-U9855G2ZPR; U9855G2ZPR; CHEMBL197603; KIN001-111; N-(4-{1-[4-(4-Acetylpiperazin-1-Yl)-Trans-Cyclohexyl]-4-Amino-1h-Pyrazolo[3,4-D]pyrimidin-3-Yl}-2-Methoxyphenyl)-1-Methyl-1h-Indole-2-Carboxamide; A 770041; Kinome_3267; 2c0o; MLS006010241; CHEMBL1970879; SCHEMBL15705796; CHEBI:91457; MolPort-039-139-535; C34H39N9O3; 3413AH; ZINC14210723; BDBM50175196; ABP001109; AKOS030526954; ZINC253387967; CS-0057; NCGC00386613-01; NCGC00346955-01; SMR004701317; HY-11011; L2G; 1H-Indole-2-carboxamide, N-(4-(1-(trans-4-(4-

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

A-432411

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Investigative

Compound Info

Synonyms

43A; (3Z)-6-(4-HYDROXY-3-METHOXYPHENYL)-3-(1H-PYRROL-2-YLMETHYLENE)-1,3-DIHYDRO-2H-INDOL-2-ONE; 2ayp; indolinone analog 13; A-432411; CHEMBL202930; SCHEMBL6674605; BDBM14649; DB07078; 29690-EP2311842A2; 29690-EP2289868A1; 29690-EP2289894A2; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-indol-2-one

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Activity

IC50 ~ 50000 nM

[3]

Compound Name

1-[5-Tert-Butyl-3-({4-[2-(Dimethylamino)ethyl]-5-Oxo-1,4-Diazepan-1-Yl}carbonyl)thiophen-2-Yl]-3-(2,3-Dichlorophenyl)urea

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Investigative

Compound Info

Synonyms

CHEMBL1929238; SCHEMBL3546033; BDBM50359359; Q27464299

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Activity

IC50 = 50000 nM

[4]

Compound Name

N-(4-(4-Amino-7-(3-(diethylamino)prop-1-enyl)thieno[3,2-c]pyridin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL232542; SCHEMBL3532542; SCHEMBL3535405; BDBM50202734

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Activity

IC50 ~ 50000 nM

[5]

Compound Name

Ethyl 3-oxo-3-[[3-[5-(3-phenoxyprop-1-ynyl)thiophen-3-yl]-1,4-dihydroindeno[1,2-c]pyrazol-5-yl]amino]propanoate

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Investigative

Compound Info

Synonyms

CHEMBL395427; BDBM50209156

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Activity

IC50 ~ 50000 nM

[6]

Compound Name

4-Amino-5-(4-phenoxyphenyl)-7-(2-aminoethyl)-7H-pyrrolo[2,3-d]pyrimidine

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Investigative

Compound Info

Synonyms

CHEMBL416444; BDBM50114584; 7-(2-Amino-ethyl)-5-(4-phenoxy-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine

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Activity

IC50 ~ 50000 nM

[7]

Compound Name

5-[(E)-2-(2-Chloropyrimidin-4-yl)vinyl]-6-phenylimidazo[2,1-b][1,3]thiazole

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Investigative

Compound Info

Synonyms

CHEMBL501444; SCHEMBL4770215; BDBM50272074; (E/Z)-5-(2-(2-chloropyrimidin-4-yl)vinyl)-6-phenylimidazo[2,1-b]thiazole; 5-[(E)-2-(2-chloropyrimidin-4-yl)ethenyl]-6-phenylimidazo[2,1-b][1,3]thiazole

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Activity

IC50 = 55000 nM

[8]

Compound Name

(E/Z)-4-(2-(4-Phenyl-1H-pyrazol-5-yl)vinyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL500929; BDBM50272161

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Activity

IC50 = 64000 nM

[8]

Compound Name

(E/Z)-N-Phenyl-4-(2-(6-phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL526932; SCHEMBL4775072; BDBM50272071; N-phenyl-4-[(E)-2-(6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine; N-Phenyl-4[(E)-2-(6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)vinyl]pyrimidin-2-amine

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Activity

IC50 = 68000 nM

[8]

Compound Name

{5-[(E)-2-(2-Aminopyrimidin-4-yl)vinyl]-4-phenyl-1H-imidazol-1-yl}acetic acid

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Investigative

Compound Info

Synonyms

CHEMBL451173; SCHEMBL4769183; BDBM50272218; (E/Z)-2-(5-(2-(2-aminopyrimidin-4-yl)vinyl)-4-phenyl-1H-imidazol-1-yl)acetic acid; 2-[5-[(E)-2-(2-aminopyrimidin-4-yl)ethenyl]-4-phenylimidazol-1-yl]acetic acid

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Activity

IC50 = 68000 nM

[8]

Compound Name

4-[(E)-2-(1-Methyl-2-phenylindol-3-yl)ethenyl]pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL527111; BDBM50272160; (E/Z)-4-(2-(1-methyl-2-phenyl-1H-indol-3-yl)vinyl)pyrimidin-2-amine

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Activity

IC50 = 83000 nM

[8]

Compound Name

2-(6-Amino-9H-purine-9-yl)-1-(1H-indole-3-yl)ethanone

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Investigative

Compound Info

Synonyms

CHEMBL521155; BDBM50268223

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Activity

IC50 = 85000 nM

[9]

Compound Name

2-(6-Amino-7H-purine-7-yl)-1-(1H-indole-3-yl)ethanone

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Investigative

Compound Info

Synonyms

CHEMBL485246; BDBM50268224

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Activity

IC50 = 95000 nM

[9]

Compound Name

N-(1-Phenylethyl)-4-(2-(6-phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL502803; SCHEMBL4769687; SCHEMBL4769691; BDBM50272070; N-(1-phenylethyl)-4-[(E)-2-(6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine; N-(1-phenylethyl)-4-[(E)-2-(6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)vinyl]pyrimidin-2-amine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

4-(2-(1-Methyl-4-phenyl-1H-imidazol-5-yl)cyclopropyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL526880; BDBM50272308

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

2-Amino-N-(1-methyl-4-phenyl-1H-imidazol-5-yl)pyrimidine-4-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL525048; BDBM50272268

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

(E/Z)-4-(2-(3-Phenylthiophen-2-yl)vinyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL500930; BDBM50272162

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

4-N-(3-Methyl-5-phenylimidazol-4-yl)pyrimidine-2,4-diamine

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Investigative

Compound Info

Synonyms

CHEMBL525047; BDBM50272266; (E/Z)-N4-(1-methyl-4-phenyl-1H-imidazol-5-yl)pyrimidine-2,4-diamine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

N-(2-Aminopyrimidin-4-yl)-1-methyl-4-phenyl-1H-imidazole-5-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL500152; BDBM50272267

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[2-(triazol-1-yl)ethoxy]quinazolin-4-amine

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Investigative

Compound Info

Synonyms

ZD-4190; ZD4190; SCHEMBL173259; BDBM4651; CHEMBL281872; BCP30854; ZINC1490292; HY-U00002; s6543; CS-6801; ZD 4190;ZD4190

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Activity

IC50 ~ 100000 nM

[10]

Compound Name

4-(2-(1-Methyl-4-phenyl-1H-imidazol-5-ylamino)ethyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL499863; BDBM50272307

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

(E/Z)-4-(2-(2-Phenylthiophen-3-yl)vinyl)pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL499883; BDBM50272214

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

4-[(E)-2-(6-Methylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL444654; BDBM50272588; (E/Z)-4-(2-(6-methylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

2-[(E)-2-(6-Phenylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

CHEMBL527110; BDBM50272158; (E/Z)-2-(2-(6-phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-4-amine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

N4-((1-Methyl-4-phenyl-1H-imidazol-5-yl)methyl)pyrimidine-2,4-diamine

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Investigative

Compound Info

Synonyms

CHEMBL450886; BDBM50272269

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

4-[(E)-2-(6-Chloroimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL507202; BDBM50272589; (E/Z)-4-(2-(6-chloroimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

4-[(E)-2-(1-Methyl-5-phenylimidazol-4-yl)ethenyl]pyrimidin-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL453195; BDBM50272216; (E/Z)-4-(2-(1-methyl-5-phenyl-1H-imidazol-4-yl)vinyl)pyrimidin-2-amine

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

5-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3358966

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Activity

IC50 ~ 100000 nM

[11]

Click to Show/Hide the Information of All Poor Binders

Non Binders of This Target (in total, 2 non binders)

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Compound Name

4-Phenyl-[1]benzofuro[2,3-b]pyridine-3,6-diol

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Investigative

Compound Info

Synonyms

CHEMBL2163772; BDBM50395892

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Activity

Ki > 1000000 nM

[12]

Compound Name

N-(4-Methoxybenzyl)benzofuro[2,3-b]pyridin-4-amine

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Investigative

Compound Info

Synonyms

CHEMBL1290072; BDBM50331612

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Activity

Ki > 1000000 nM

[13]

References

Top

REF 1

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. ACS Med Chem Lett. 2010 Sep 7;1(9):454-9.

REF 2

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22.

REF 3

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):421-6.

REF 4

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). Bioorg Med Chem Lett. 2011 Dec 1;21(23):7155-65.

REF 5

Discovery of thienopyridines as Src-family selective Lck inhibitors. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1167-71.

REF 6

Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3136-40.

REF 7

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1683-6.

REF 8

Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4723-6.

REF 9

Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors. Eur J Med Chem. 2009 Apr;44(4):1788-93.

REF 10

Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. J Med Chem. 2002 Mar 14;45(6):1300-12.

REF 11

Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor (PDGF-R) guided by water thermodynamics. J Med Chem. 2015 Jan 8;58(1):170-82.

REF 12

Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6914-8.

REF 13

Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6915-9.

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