Target Poor or Non Binder(s) Information

Target General Information

Target ID

T73756

Target Info

Target Name

Ephrin type-B receptor 2 (EPHB2)

Synonyms

hEK5; Tyrosine-protein kinase receptor EPH-3; Tyrosine-protein kinase TYRO5; TYRO5; Renal carcinoma antigen NY-REN-47; Receptor protein-tyrosine kinase HEK5; EphB2 receptor tyrosine kinase; EphB2; EPTH3; EPHT3; EPH-like kinase 5; EPH tyrosine kinase 3; ELK-related tyrosine kinase; EK5; Developmentally-regulated Eph-related tyrosine kinase; DRT

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Target Type

Clinical trial Target

Gene Name

EPHB2

Biochemical Class

Kinase

UniProt ID

P29323

Poor Binders of This Target (in total, 11 binders)

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Compound Name

ISIS-CRP

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Phase 1

Compound Info

Synonyms

1-(Tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 172889-27-9; pp2; PP 2; 1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; AG 1879; 1-tert-butyl-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; PP2; 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine; AG-1879; CHEMBL406845; CHEBI:78331; AK-60369; 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine; 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C15H16ClN5; 1qpe; 4few; PBBRWFOVCUAONR-UHFFFAOYSA-N; AG1879; PP 2 (AG 1879)

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Activity

IC50 = 52000 nM

[1]

Compound Name

Src kinase inhibitor I

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Investigative

Compound Info

Synonyms

Src Kinase Inhibitor I; 179248-59-0; Src I1; Src Inhibitor 1; Src I 1; Src Inhibitor-1; Src-l1; 6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine; SKI-1; CHEMBL97771; CHEBI:78332; 6,7-dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine; 4-Quinazolinamine, 6,7-dimethoxy-N-(4-phenoxyphenyl)-; 4-(4'-PHENOXYANILINO)-6,7-DIMETHOXYQUINAZOLINE; -Phenoxyanilino)-6,7-dimethoxyquinazoline; Src-I1; AC1LT1HN; Bionet1_003516; Oprea1_231056; GTPL6042; SCHEMBL1387206; KS-00002WRA; HMS578L18; CTK0E3319; AOB5689; DTXSID50363056

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Activity

IC50 = 86000 nM

[1]

Compound Name

AG 1296

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Investigative

Compound Info

Synonyms

tyrphostin AG-1296; AG-1296; AG1296

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Activity

IC50 = 110000 nM

[1]

Compound Name

PD-174265

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Investigative

Compound Info

Synonyms

pd 174265; 4-aminoquinazoline, 2a; PD-174265; CHEMBL188762; 4-[(3-Bromophenyl)amino]-6-propionylamidoquinazoline; N-{4-[(3-Bromophenyl)amino]quinazolin-6-Yl}propanamide; 3lok; 2hwp; AC1L1IS1; BMC163482 Compound 3; GTPL6017; SCHEMBL2944459; BDBM31826; WUPUZEMRHDROEO-UHFFFAOYSA-N; MolPort-044-561-456; HMS3229I05; ZINC1488953; IN1163; HSCI1_000122; CCG-206770; ACM216163530; N-[4-(3-bromoanilino)quinazolin-6-yl]propanamide; J-014179; N-(4-(3-bromophenylamino)quinazolin-6-yl)propionamide

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Activity

IC50 = 180000 nM

[1]

Compound Name

2-{3-[(5E)-5-{[(2,3-Dichlorophenyl)carbamoyl]imino}-3-thiophen-2-yl-2,5-dihydro-1H-pyrazol-1-yl]phenyl}acetamide

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Investigative

Compound Info

Synonyms

CHEMBL1269839; DP-1376; SCHEMBL2082516; BDBM50328772; Q27459911

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

3-(4-Chloro-phenyl)-1-[2-(5-fluoro-2-methyl-1H-indol-3-yl)-ethyl]-1-pyridin-4-ylmethyl-thiourea

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Investigative

Compound Info

Synonyms

CHEMBL191403; BDBM50166045; ZINC13283372; MCULE-8323990659; N'-(4-chlorophenyl)-N-[2-(5-fluoro-2-methyl-1H-indol-3-yl)ethyl]-N-(pyridin-4-ylmethyl)thiourea

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Activity

IC50 = 65000 nM

[1]

Compound Name

4-Chloro-N-(2-phenylimidazo[1,2-a]pyrimidin-3-yl)benzamide

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Investigative

Compound Info

Synonyms

CHEMBL426989; 4-chloro-N-{2-phenylimidazo[1,2-a]pyrimidin-3-yl}benzamide; IFLab1_000450; Cambridge id 5856609; Oprea1_048451; HMS1413E10; ZINC444939; BDBM50166044; STK822525; ZINC00444939; AKOS001610938; MCULE-9418897241; IDI1_008669; SR-01000388417; SR-01000388417-1; F0170-0339; Z275251722; 4-Chloro-N-(2-phenyl-imidazo[1,2-a]pyrimidin-3-yl)-benzamide

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Activity

IC50 = 88000 nM

[1]

Compound Name

N-{5-[1-(2-Amino-4-methyl-thiazol-5-yl)-eth-(E)-ylidene-hydrazinocarbonyl]-4-methyl-thiazol-2-yl}-benzenesulfonamide

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Investigative

Compound Info

Synonyms

CHEMBL192044; BDBM50166036; ZINC100818888

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Activity

IC50 = 94000 nM

[1]

Compound Name

3-(4-Fluoro-phenyl)-1-[2-(2-methyl-1H-indol-3-yl)-ethyl]-1-pyridin-4-ylmethyl-thiourea

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Investigative

Compound Info

Synonyms

CHEMBL191630; BDBM50166038; ZINC13283339; MCULE-6753242652; N'-(4-fluorophenyl)-N-[2-(2-methyl-1H-indol-3-yl)ethyl]-N-(pyridin-4-ylmethyl)thiourea

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Activity

IC50 = 104000 nM

[1]

Compound Name

N-(Pyridin-2-ylmethyl)-7H-purin-6-amine

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Investigative

Compound Info

Synonyms

CHEMBL365356; SMR000017626; N-(pyridin-2-ylmethyl)-9H-purin-6-amine; Oprea1_708615; MLS000101214; SCHEMBL9225653; SCHEMBL17933798; purin-6-yl(2-pyridylmethyl)amine; HMS2248H22; ZINC2719609; BDBM50166039; STK944576; AKOS001396305; AKOS005858063; MCULE-2424903635; SDCCGMLS-0065419.P001; NCGC00081762-02; NCGC00168495-01; (9H-Purin-6-yl)-pyridin-2-ylmethyl-amine; ST50139380; N-[(pyridin-2-yl)methyl]-7H-purin-6-amine; Z372960568

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Activity

IC50 = 106000 nM

[1]

Compound Name

N-(2-Methoxyphenyl)-2-[(5-methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]acetamide

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Investigative

Compound Info

Synonyms

CHEMBL191636; Oprea1_102485; Oprea1_358229; HMS1917D11; ZINC716554; BDBM50166046; CCG-96533; STK125983; AKOS000713486; MCULE-2259215585; NCGC00141194-01; EU-0081462; AG-205/37217010; SR-01000432548; SR-01000432548-1

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Activity

IC50 = 136000 nM

[1]

Click to Show/Hide the Information of All Poor Binders

Non Binders of This Target (in total, 4 non binders)

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Compound Name

3-[3-(2-Fluoro-phenyl)-[1,2,4]oxadiazol-5-yl]-N-(3-isopropoxy-propyl)-propionamide

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Investigative

Compound Info

Synonyms

CHEMBL193115; ZINC4921545; BDBM50166047; MCULE-5264982401; 3-[3-(2-fluorophenyl)-1,2,4-oxadiazol-5-yl]-N-(3-isopropoxypropyl)propanamide

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Activity

IC50 = 201000 nM

[1]

Compound Name

5-[(Z)-1-(3,4-Dimethoxyphenyl)methylidene]-2-(4-hydroxyanilino)-1,3-thiazol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL362977; ZINC4567489; BDBM50166042; STK589596; STK974198; STL494421; AKOS001669945; AKOS002213095; AKOS002529799; AKOS005512007; BIM-0039511.P001; ST50054900; (Z)-5-(3,4-dimethoxybenzylidene)-2-((4-hydroxyphenyl)amino)thiazol-4(5H)-one

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Activity

IC50 = 220000 nM

[1]

Compound Name

5-[1-Furan-2-yl-meth-(Z)-ylidene]-2-(4-methoxy-phenylamino)-thiazol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL365327; MLS000769550; cid_1836529; HMS2785G07; ZINC9329535; BDBM50166037; STK849880; AKOS001670008; AKOS002213123; AKOS005628941; AKOS016868413; SMR000434280; ST50054917; SR-01000112056; SR-01000112056-1; 5-(2-furylmethylene)-2-[(4-methoxyphenyl)amino]-1,3-thiazolin-4-one; (5Z)-5-(2-furylmethylene)-2-[(4-methoxyphenyl)amino]-1,3-thiazol-4(5H)-one

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Activity

IC50 = 230000 nM

[1]

Compound Name

3-(4-Methoxy-phenyl)-1-[2-(2-methyl-1H-indol-3-yl)-ethyl]-1-pyridin-4-ylmethyl-thiourea

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Investigative

Compound Info

Synonyms

CHEMBL193891; BDBM50166043; ZINC13283336; MCULE-5464890900; N'-(4-methoxyphenyl)-N-[2-(2-methyl-1H-indol-3-yl)ethyl]-N-(pyridin-4-ylmethyl)thiourea

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Activity

IC50 = 250000 nM

[1]

References

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REF 1

Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening. J Med Chem. 2005 May 5;48(9):3221-30.

REF 2

Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5793-8.

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