Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T73694 | Target Info | |||
| Target Name | Tyrosine-protein kinase BRK (PTK6) | ||||
| Synonyms |
Protein-tyrosine kinase 6; Breast tumor kinase; BRK
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| Target Type | Clinical trial Target | ||||
| Gene Name | PTK6 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(7-Methoxyquinolin-6-yl)thieno[3,2-d]pyrimidine-7-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL357756; CHEMBL3822972; BDBM206104; DB-085143; US9255110, 17
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2R)-2,3-dihydroxypropyl]-4-methoxybenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1949788; SCHEMBL12134179; BDBM50364832; CH-4932748
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
[6-Chloro-4-methyl-3-[[3-(methylsulfamoylamino)phenyl]methyl]-2-oxochromen-7-yl] N,N-dimethylcarbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3086065; SCHEMBL959662; BDBM50443366
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-[(E)-2-(4-Chlorophenyl)ethenyl]-N-[(2S)-2,3-dihydroxypropyl]-4-methoxybenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1949789; SCHEMBL12134185; BDBM50364833; CH-4932750
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(R)-6-(1-(2,6-Dichloro-3-fluorophenyl)ethoxy)quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL600795; BDBM50306683
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
2-(6-((R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy)quinolin-3-yl)cyclopropanecarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL602472; BDBM50306684; CH-5234152
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
5-[(5-Chloro-3-ethoxy-2-hydroxyphenyl)methylideneamino]-1,3-dihydrobenzimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3335237; BDBM50026050
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| Activity |
IC50 = 51250 nM
|
[5] | |||
| Compound Name |
Tyrphostin AG 808
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Investigative | Compound Info | ||
| Synonyms |
NSC650934; AG-808; (E)-2-(3,4-dihydroxybenzoyl)-3-(1H-indol-3-yl)prop-2-enenitrile; Tyrphostin AG-808; Lopac-T-5318; Lopac0_001178; CHEMBL68534; Indole-Containing Inhibitor 5; BDBM5171; Tyrphostin AG 808, >=98%; DTXSID401017668; ZINC3927328; CCG-205252; NSC-650934; 2-Propenenitrile,4-dihydroxy- benzoyl)-; NCGC00016030-01; NCGC00016030-02; NCGC00016030-03; NCGC00016030-04; NCGC00094433-01; NCGC00094433-02; EU-0101178; T 5318; SR-01000076162; SR-01000076162-1; 2-(3,4-Dihydroxybenzoyl)-3-(1H-indol-3-yl)acrylonitrile; 2-Propenenitrile, 3-(1H-indol-3-yl)-2-(3,4-dihydroxy- benzoyl)-; 2-Cyano-3-(3',4'-dihydroxyphenyl)-1-(3'-indolyl)-3-oxo-1-propene; (2E)-2-[(3,4-dihydroxyphenyl)carbonyl]-3-(1H-indol-3-yl)prop-2-enenitrile
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| Activity |
IC50 = 53240 nM
|
[5] | |||
| Compound Name |
5-[(2-Hydroxy-5-iodo-3-methoxyphenyl)methylideneamino]-1,3-dihydrobenzimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3335234; BDBM50025873
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| Activity |
IC50 = 58100 nM
|
[5] | |||
| Compound Name |
5-[(5-Chloro-2-hydroxy-3-methoxyphenyl)methylideneamino]-1,3-dihydrobenzimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3335233; CBDivE_005149; Oprea1_402787; BDBM50025876; 5-[(5-Chloro-2-hydroxy-3-methoxybenzylidene)amino]-1,3-dihydro-2H-benzimidazol-2-one
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| Activity |
IC50 = 74040 nM
|
[5] | |||
| Compound Name |
5-{[(5-Bromo-2-hydroxyphenyl)methylidene]amino}-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3335225; Oprea1_558293; ZINC3233546; BDBM50025916; STL507490; AKOS001011519; MCULE-6417148311; ST51019730; SR-01000033313; SR-01000033313-1; Z56833971; 5-[(1E)-2-(5-bromo-2-hydroxyphenyl)-1-azavinyl]-3-hydrobenzimidazol-2-one
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 6 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(1H-Pyrido[2,3-b]indole-4-yl)-4-chloroaniline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133823
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
3-[6-(Morpholinosulfonyl)-1H-pyrido[2,3-b]indole-4-ylamino]phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133824
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
N-(1H-Pyrido[2,3-b]indole-4-yl)-o-toluidine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133820
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
3-(6-Acetyl-1H-pyrido[2,3-b]indole-4-ylamino)phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133816
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|
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
3-[[6-[4-(2-Hydroxyethyl)piperazin-1-yl]sulfonyl-9H-pyrido[2,3-b]indol-4-yl]amino]phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133832
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|
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
3-(6-Bromo-1H-pyrido[2,3-b]indole-4-ylamino)phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3133833
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|
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of a selective inhibitor of transforming growth factor -activated kinase 1 by biosensor-based screening of focused libraries. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1031-1036. | ||||
| REF 2 | Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. Bioorg Med Chem. 2012 Feb 15;20(4):1442-60. | ||||
| REF 3 | The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6223-7. | ||||
| REF 4 | Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1405-9. | ||||
| REF 5 | Discovery of (E)-5-(benzylideneamino)-1H-benzo[d]imidazol-2(3H)-one derivatives as inhibitors for PTK6. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4659-4663. | ||||
| REF 6 | Novel inhibitors of breast cancer relevant kinases Brk and HER2. Medchemcomm. 2014;5:659-64. | ||||
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