Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T68163 | Target Info | |||
| Target Name | Tyrosine-protein kinase Lyn (JTK8) | ||||
| Synonyms |
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
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| Target Type | Clinical trial Target | ||||
| Gene Name | LYN | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 18 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
ABT-869
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Phase 3 | Compound Info | ||
| Synonyms |
Linifanib; ABT 869; S1003_Selleck; AL-39324; RG-3635; ABT869, Linifanib, AL-39324, RG3635; N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N1-(2-fluoro-5-methylphenyl)urea; N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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
|
[2] | |||
| Compound Name |
Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
WYE-354; WYE 354; pyrazolo pyrimidine, 19; cc-506; MLS006011008; SCHEMBL300431; CHEMBL561708; GTPL9361; WYE354; BDBM35587; DTXSID00657912; C24H29N7O5; HMS3654N09; BCP02898; ZINC43013490; CCG-264882; CS-0183; SB19260; NCGC00242484-01; NCGC00242484-02; NCGC00242484-09; AC-28454; AS-55957; HY-12034; SMR004702806; BCP0726000260; DB-059456; FT-0675866; S1266; SW219671-1; X7422; W-5702; J-001552; J-514253; BRD-K77008974-001-01-6; Q27166532; mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| 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
|
[4] | |||
| Compound Name |
Methyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095626; SCHEMBL3984085; BDBM50316252; methyl 4-[6-(4-aminophenyl)-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| 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
|
[6] | |||
| Compound Name |
(E)-N-(4-Chloroimidazo[1,5-a]quinoxalin-8-yl)-4-(dimethylamino)-N-methylbut-2-enamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1916719; BDBM50357320
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| 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
|
[4] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-(3-chlorophenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 51; SCHEMBL420822; CHEMBL269884; BDBM21105; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-(3-chlorophenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
2-(2-Methoxy-ethoxy)-N-{3-[5-(3-phenoxy-prop-1-ynyl)-thiophen-3-yl]-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl}-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL245968; BDBM50209144
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
2-(4-Methyl-piperazin-1-yl)-N-{3-[5-(3-phenoxy-prop-1-ynyl)-thiophen-3-yl]-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl}-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL245377; SCHEMBL4820003; BDBM50209158
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| Activity |
IC50 ~ 50000 nM
|
[8] | |||
| Compound Name |
Tert-Butyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095627; SCHEMBL3991434; BDBM50316253
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
6-Methyl-4-(4-methyl-1H-indol-5-ylamino)-5-(3-(4-methylpiperazin-1-ylsulfonyl)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1080995; SCHEMBL2934911; BDBM50311954
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-[3-(trifluoromethyl)phenyl]urea
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Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 50; SCHEMBL425740; CHEMBL430090; BDBM21104; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-[3-(trifluoromethyl)phenyl]urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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
|
[8] | |||
| Compound Name |
3-[4-(3-Amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-1-(2-fluoro-5-methylphenyl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
Aminobenzoisoxazole, 49; SCHEMBL419044; CHEMBL270084; BDBM21103; 1-[4-(3-amino-7-methoxy-1,2-benzoxazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-(1H-Indole-4-ylamino)-5-[3-[2-(4-methylpiperazino)ethoxy]phenyl]pyridine-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL467321; SCHEMBL2971392; BDBM29824; 4-indolylamino-5-phenyl-3-pyridinecarbonitrile, 12d; 4-(1H-indol-4-ylamino)-5-[3-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]pyridine-3-carbonitrile
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
6-(1,9-Diazaspiro[5.5]undecan-9-Yl)-9h-Purine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420909; BDBM50439464; 9-(9H-purin-6-yl)-1,9-diazaspiro[5.5]undecane; Q27465376; SIJ
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| Activity |
IC50 = 178000 nM
|
[11] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 15 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
HARMINE
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|
Patented | Compound Info | ||
| Synonyms |
Harmine; 442-51-3; 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole; Banisterine; Leucoharmine; Telepathine; Yageine; Yajeine; 7-Methoxy-1-methyl-9H-beta-carboline; 9H-Pyrido[3,4-b]indole, 7-methoxy-1-methyl-; Telepathin; Banisterin; Yagein; Harmin; 1-Methyl-7-methoxy-beta-carboline; UNII-4FHH5G48T7; 7-Methoxy-1-methyl-9H-pyrido(3,4-b)indole; Harmin hydrochloride; Harmine, 98%; Banisterine monohydrate; EINECS 207-131-4; 9H-Pyrido(3,4-b)indole, 7-methoxy-1-methyl-; BRN 0178813; 4FHH5G48T7; C13H12N2O; CHEBI:28121; 7-METHOXY-1-METHYL-9H-BETA-CARBOLINE
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| Activity |
IC50 > 250000 nM
|
[12] | |||
| Compound Name |
Y-c[D-Pen-(2')Nal-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL405681; BDBM50064832
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-D-(2')Nal-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL404595; BDBM50064829
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216490; Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(2R,3R)-2-Me-(2')Nal-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL412218; BDBM50064828
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL436961; Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(2R,3S)-2-Me-(2')Nal-GSFC]KR-NH2
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL262212; BDBM50064837
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(2S,3R)-2-Me-(2')Nal-GSFC]KR-NH2
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL413670; BDBM50064847
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
Y-c[D-Pen-(2S,3S)-2-Me-(2')Nal-GSFC]KR-NH2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL414159; BDBM50064843
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| Activity |
IC50 > 800000 nM
|
[13] | |||
| Compound Name |
1-(5-Methyl-1H-imidazol-4-yl)-9H-beta-carboline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL273547; BDBM50111434; 1-(5-Methyl-1H-imidazole-4-yl)-beta-carboline
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| Activity |
IC50 > 250000 nM
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[12] | |||
| Compound Name |
1-(2-Chloro-5-nitro-phenyl)-9H-beta-carboline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL14217; SCHEMBL17102963; BDBM50111433; 1-(2-Chloro-5-nitrophenyl)-beta-carboline; 1-(2-chloro-5-nitro-phenyl)-beta-carboline; 1-(2-chloro-5-nitrophenyl)-9H-pyrido[3,4-b]indole
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| Activity |
IC50 > 250000 nM
|
[12] | |||
| Compound Name |
7-Fluoro-1-methyl-9H-pyrido[3,4-b]indole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL14445; 1-Methyl-7-fluoro-beta-carboline; BDBM50111435; 7-Fluoro-1-methyl-9H-beta-carboline
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| Activity |
IC50 > 250000 nM
|
[12] | |||
| Compound Name |
N-(1-(3-Amino-3-oxopropyl)-5-(N-ethylcyclohexanecarboxamido)-1H-benzo[d]imidazol-2-yl)-4-cyanobenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL458787; BDBM50274709
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|
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| Activity |
IC50 > 1000000 nM
|
[14] | |||
| Compound Name |
N-(1-(3-(1H-Imidazol-1-yl)propyl)-5-(N-methylcyclohexanecarboxamido)-1H-benzo[d]imidazol-2-yl)-4-cyanobenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL485031; BDBM50274669
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| Activity |
IC50 > 1000000 nM
|
[14] | |||
| Compound Name |
N-(1-(3-Amino-3-oxopropyl)-5-(N-methylcyclohexanecarboxamido)-1H-benzo[d]imidazol-2-yl)-4-chlorobenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL483403; BDBM50274340
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| Activity |
IC50 > 1000000 nM
|
[14] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases. J Med Chem. 2008 Mar 13;51(5):1231-41. | ||||
| REF 2 | 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 3 | ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines. J Med Chem. 2009 Aug 27;52(16):5013-6. | ||||
| REF 4 | 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 5 | Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. J Med Chem. 2009 Dec 24;52(24):8010-24. | ||||
| REF 6 | 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 7 | Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6258-63. | ||||
| REF 8 | 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 9 | Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6575-7. | ||||
| REF 10 | Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles. Bioorg Med Chem Lett. 2009 May 1;19(9):2461-3. | ||||
| REF 11 | Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. Bioorg Med Chem. 2013 Sep 15;21(18):5707-24. | ||||
| REF 12 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1129-32. | ||||
| REF 13 | Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographica... J Med Chem. 1998 Jun 18;41(13):2252-60. | ||||
| REF 14 | Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk). Bioorg Med Chem Lett. 2008 Oct 15;18(20):5545-9. | ||||
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