Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T74312 | Target Info | |||
| Target Name | Fms-like tyrosine kinase 3 (FLT-3) | ||||
| Synonyms |
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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| Target Type | Successful Target | ||||
| Gene Name | FLT3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 18 binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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 ~ 100000 nM
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[1] | |||
| Compound Name |
NSC-73306
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
1-Cyclohexyl-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-h][1,6]naphthyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2322140; SCHEMBL9989432; BDBM50426740; ZINC95583901; DB-103199; 1-cyclohexyl-2,3,4,7-tetrahydropyrrolo[2,3-h][1,6]naphthyridine
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| Activity |
IC50 ~ 50000 nM
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[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
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[4] | |||
| 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
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[5] | |||
| 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 |
Propan-2-yl 2-[(E)-3-acetamidoprop-1-enyl]-6-hydroxy-4-methoxybenzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3357196; BDBM50037544
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| Activity |
IC50 ~ 50000 nM
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[6] | |||
| Compound Name |
2-[9-(4-Amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]-N-(4-morpholin-4-ylphenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL395080; BDBM50218700
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| Activity |
IC50 ~ 50000 nM
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[7] | |||
| Compound Name |
N-(3-Chlorophenyl)-7-(2-chloro-2-phenylethyl)-2-methylsulfanylpyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4068876; BDBM50230313
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| Activity |
IC50 = 55000 nM
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[8] | |||
| Compound Name |
N-Benzyl-7-[(4-fluorophenyl)methyl]-2-methylsulfanylpyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4091022; BDBM50230317
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| Activity |
IC50 = 60000 nM
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[8] | |||
| Compound Name |
7-[(4-Fluorophenyl)methyl]-2-methylsulfanyl-4-piperidin-1-ylpyrrolo[2,3-d]pyrimidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4073713; BDBM50230321
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| Activity |
IC50 = 61000 nM
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[8] | |||
| Compound Name |
4-[7-[(4-Fluorophenyl)methyl]-2-methylsulfanylpyrrolo[2,3-d]pyrimidin-4-yl]morpholine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4100526; BDBM50230320
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| Activity |
IC50 = 61000 nM
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[8] | |||
| Compound Name |
7-[(4-Fluorophenyl)methyl]-2-methylsulfanyl-4-pyrrolidin-1-ylpyrrolo[2,3-d]pyrimidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4088440; BDBM50230316
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| Activity |
IC50 = 64000 nM
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[8] | |||
| Compound Name |
N-Benzyl-7-(2-chloro-2-phenylethyl)-2-methylsulfanylpyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4096164; BDBM50230315
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| Activity |
IC50 = 68000 nM
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[8] | |||
| Compound Name |
7-(2-Chloro-2-phenylethyl)-2-methylsulfanyl-N-phenylpyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4103914; BDBM50230318
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| Activity |
IC50 = 72000 nM
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[8] | |||
| Compound Name |
N-[2-(4-Chlorophenyl)ethyl]-7-[(4-fluorophenyl)methyl]-2-methylsulfanylpyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4098763; BDBM50230312
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| Activity |
IC50 = 76000 nM
|
[8] | |||
| Compound Name |
2-[(3,4-Dimethoxybenzoyl)amino]-4,5,6,7,8,9-hexahydrocycloocta[b]thiophene-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL208628; CBMicro_017738; Cambridge id 6101721; Oprea1_576159; ZINC2083933; BDBM50185108; CCG-13922; STK426697; AKOS003270100; MCULE-8469808753; BIM-0017730.P001; ST50919681; AK-968/12163652; SR-01000227657; SR-01000227657-1
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| Activity |
IC50 ~ 100000 nM
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[9] | |||
| Compound Name |
Chembl4276946
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Investigative | Compound Info | ||
| Synonyms |
GTPL9965; compound 3a [Pipionne et al, 2018]; 1-[5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl]ethan-1-one
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[[1-Cyclopentyl-5-[1-(Oxetan-3-Yl)piperidin-4-Yl]pyrazol-3-Yl]amino]pyridine-4-Carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3629013; GTPL9989; SCHEMBL22137472; BDBM50128294; AKOS032960466; compound 11 [PMID: 26431428]; Q27455367; 2-(1-Cyclopentyl-5-(1-(oxetane-3-yl)-4-piperidinyl)-1H-pyrazole-3-ylamino)pyridine-4-carbonitrile
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| Activity |
IC50 = 322000 nM
|
[11] | |||
| 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 | Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J Med Chem. 2009 May 28;52(10):3191-204. | ||||
| REF 3 | Design and synthesis of tricyclic cores for kinase inhibition. Bioorg Med Chem Lett. 2013 Feb 1;23(3):693-8. | ||||
| 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 | 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 6 | Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core. Bioorg Med Chem. 2014 Dec 1;22(23):6625-6637. | ||||
| REF 7 | Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. J Med Chem. 2007 Aug 23;50(17):4162-76. | ||||
| REF 8 | Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma. Eur J Med Chem. 2017 Feb 15;127:369-378. | ||||
| REF 9 | Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6. | ||||
| REF 10 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
| REF 11 | Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). J Med Chem. 2015 Oct 22;58(20):8182-99. | ||||
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