Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T75570 | Target Info | |||
| Target Name | Yes tyrosine kinase (YES) | ||||
| Synonyms |
p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
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| Target Type | Clinical trial Target | ||||
| Gene Name | YES1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 21 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 |
1-Tert-butyl-3-[7-(3,4-dimethoxyphenyl)-1,5-naphthyridin-2-yl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318025; SCHEMBL1932951; BDBM50050849
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| Activity |
IC50 = 85540 nM
|
[5] | |||
| Compound Name |
(4-{2-Acetylamino-2-[1-(3-carbamoyl-4-cyclohexylmethoxy-phenyl)-1-methyl-ethylcarbamoyl]-ethyl}-2-phosphono-phenoxy)-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL265777; BDBM50103781
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| Activity |
IC50 = 94500 nM
|
[6] | |||
| Compound Name |
N-(4-Morpholin-4-ylphenyl)-2-phenylpyrido[3,4-b]pyrazin-7-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780543
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(3-Ethynylphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780350
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Ethyl-3-(2-phenylpyrido[3,4-b]pyrazin-5-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3780985
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-(3-Phenylpyrido[3,4-b]pyrazin-8-yl)-3-prop-2-enylurea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781906
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N-(3-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781584
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
1-Benzyl-3-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318029; SCHEMBL1933048; BDBM50050853
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
5-[4-Amino-1-(2,2-dimethoxyethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3800138
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5-[4-Amino-1-(1,3-dioxolan-2-ylmethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797590
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
1-[7-(1-Methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]-3-phenylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318028; SCHEMBL1932302; BDBM50050854
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
5-[4-Amino-1-(2,2-diethoxyethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzoxazol-2-amine
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Investigative | Compound Info | ||
| Synonyms |
eCF309; eCF-309; eCF 309; GTPL9571; CHEMBL3800481; SCHEMBL22773819; BDBM200300; cid_122163152; AKOS030211008; ZINC585672921; compound 12 [Fraser et al., 2016]; J3.595.265I
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|
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
1-Ethyl-3-[7-(4-methoxyphenyl)-1,5-naphthyridin-2-yl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318023; SCHEMBL1932961; BDBM50050851
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|
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(4-{2-Acetylamino-2-[(S)-1-(3-carbamoyl-4-cyclohexylmethoxy-phenyl)-ethylcarbamoyl]-ethyl}-2-phosphono-phenoxy)-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL76350; BDBM50103782
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| Activity |
IC50 = 110000 nM
|
[6] | |||
| Compound Name |
[4-{2-Acetylamino-2-[(S)-1-(3-carbamoyl-4-cyclohexylmethoxy-phenyl)-ethylcarbamoyl]-ethyl}-2-(ethoxy-hydroxy-phosphoryl)-phenoxy]-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL308734; BDBM50103780
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|
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| Activity |
IC50 = 156000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 7 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(4-{2-[1-(3-Carbamoyl-4-cyclohexylmethoxy-phenyl)-1-methyl-ethylcarbamoyl]-ethyl}-2-phosphono-phenoxy)-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL433507; BDBM50103786
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|
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| Activity |
IC50 = 303000 nM
|
[6] | |||
| Compound Name |
(5-{2-[1-(3-Carbamoyl-4-cyclohexylmethoxy-phenyl)-1-methyl-ethylcarbamoyl]-ethyl}-2-hydroxy-phenyl)-phosphonic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL76937; BDBM50103788
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| Activity |
IC50 > 500000 nM
|
[6] | |||
| Compound Name |
[5-{2-[1-(3-Carbamoyl-4-cyclohexylmethoxy-phenyl)-1-methyl-ethylcarbamoyl]-ethyl}-2-(tetrazol-1-ylmethoxy)-phenyl]-phosphonic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL311114; BDBM50103778
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|
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| Activity |
IC50 > 500000 nM
|
[6] | |||
| Compound Name |
{4-[2-Acetylamino-2-(3-carbamoyl-4-cyclohexylmethoxy-benzylcarbamoyl)-ethyl]-2-phosphono-phenoxy}-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL263721; BDBM50103785
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|
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| Activity |
IC50 > 500000 nM
|
[6] | |||
| Compound Name |
Trifluoro-methanesulfonic acid 4-{2-[1-(3-carbamoyl-4-cyclohexylmethoxy-phenyl)-1-methyl-ethylcarbamoyl]-ethyl}-2-phosphono-phenyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL430825; BDBM50103779
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|
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| Activity |
IC50 > 500000 nM
|
[6] | |||
| Compound Name |
(4-{2-Acetylamino-2-[(S)-1-(3-carbamoyl-4-cyclohexylmethoxy-phenyl)-ethylcarbamoyl]-ethyl}-phenoxy)-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL75182; BDBM50103787
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|
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| Activity |
IC50 > 500000 nM
|
[6] | |||
| Compound Name |
{4-[2-Acetylamino-2-(3-carbamoyl-4-cyclohexylmethoxy-phenylcarbamoyl)-ethyl]-2-phosphono-phenoxy}-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL308164; BDBM50103783
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|
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| Activity |
IC50 > 500000 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 (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52. | ||||
| REF 6 | A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2319-23. | ||||
| REF 7 | Efficient synthesis of novel disubstituted pyrido[3,4-b]pyrazines for the design of protein kinase inhibitors. Medchemcomm. 2016;7:224-9. | ||||
| REF 8 | eCF309: a potent, selective and cell-permeable mTOR inhibitor. Medchemcomm. 2016;7:471-7. | ||||
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