Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T00852 | Target Info | |||
| Target Name | Serine/threonine-protein kinase cot (COT) | ||||
| Synonyms |
Tumor progression locus 2; TPL-2; Proto-oncogene c-Cot; Mitogen-activated protein kinase kinase kinase 8; ESTF; Cancer Osaka thyroid oncogene; COT
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| Target Type | Clinical trial Target | ||||
| Gene Name | MAP3K8 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 20 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Thieno[2,3-c]pyridine-2-carboxamide,4-([1,1'-biphenyl]-4-yloxy)-
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Investigative | Compound Info | ||
| Synonyms |
thieno[2,3-c]pyridine, 6; CHEMBL518731; BDBM28041; ZINC34043279; 4-(4-phenylphenoxy)thieno[2,3-c]pyridine-2-carboxamide
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-(4-(4-Iodophenoxy)thieno[2,3-c]pyridin-2-yl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL496947; BDBM50265241
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-(4-Iodophenoxy)thieno[2,3-c]pyridin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL526374; thieno[2,3-c]pyridin-2-amine,4-(4-iodophenoxy)-; 4-(4-iodo-phenoxy)-thieno[2,3-c]pyridin-2-ylamine; SCHEMBL5553958; BDBM50265240; ZINC40425019
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-({2-[(3-Hydroxyphenyl)amino]pyrimidin-4-YL}amino)benzamide
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Investigative | Compound Info | ||
| Synonyms |
DB07268; DB-07268; 2-((2-((3-Hydroxyphenyl)amino)pyrimidin-4-yl)amino)benzamide; 4-(2-carbamoylanilino)-2-(3-hydroxyanilino)pyrimidine; 4-anilinopyrimidine 2b; CHEMBL242237; BDBM15978; BCP16456; EX-A2356; MFCD26960941; s6740; ZINC14960224; AKOS027439962; CS-1562; NCGC00378943-01; NCGC00378943-02; AS-56032; DB 07268; HY-15737; Q27096495; 2-[[2-(3-hydroxyanilino)pyrimidin-4-yl]amino]benzamide; 2-(4-(3-hydroxyphenylamino)pyrimidin-2-ylamino)benzamide
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[3-(2-Pyridin-4-ylpyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-3-(trifluoromethyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1089082; SCHEMBL4656083; BDBM50314051; N-(3-(2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamide
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
2-[6-[4-(Methylcarbamoyl)phenyl]thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836723; BDBM50354557
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
N-[[4-Methyl-5-[3-(2H-tetrazol-5-yl)-1H-indazol-5-yl]pyridin-3-yl]methyl]ethanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808583; SCHEMBL6508637; BDBM50349463; Ethyl-{4-methyl-5-[3-(1H-tetrazol-5-yl)-1H-indazol-5-yl]-pyridin-3-ylmethyl}-amine
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[6-(5-Chlorothiophen-2-yl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836729; BDBM50354561
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
5-(3-(1H-Benzo[D]imidazol-2-YL)-1H-indazol-5-YL)-4-methylpyridin-3-OL
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808595; SCHEMBL5516248; DTXSID30432613; BDBM50349475; MFCD18711506
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
5-[3-(1H-Benzimidazol-2-yl)-1H-indazol-5-yl]-4-methylpyridine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808593; SCHEMBL5516430; BDBM50349473
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
5-[3-(1H-Benzimidazol-2-yl)-1H-indazol-5-yl]-N,4-dimethylpyridin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808592; BDBM50349472
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Ethyl 2-[6-(4-chlorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836725; BDBM50354558
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
4-[[5-[3-(1H-Benzimidazol-2-yl)-1H-indazol-5-yl]-4-methylpyridin-3-yl]methyl]morpholine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808596; SCHEMBL5514168; BDBM50349476
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[[6-(4-Chlorophenyl)thieno[3,2-d]pyrimidin-4-yl]amino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836642; BDBM50354563
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-[[6-(4-Chlorophenyl)thieno[3,2-d]pyrimidin-4-yl]-methylamino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836643; BDBM50354564
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
3-(1H-Benzimidazol-2-yl)-5-(4,5-dimethylpyridin-3-yl)-1H-indazole
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808594; SCHEMBL5515599; BDBM50349474
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[6-(4-Methylpiperidin-1-yl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836636; BDBM50354562
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| 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
|
[7] | |||
| Compound Name |
5-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3358966
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-[6-(4-Phenylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1836720; BDBM50354556
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|
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1722-5. | ||||
| REF 2 | Discovery of thieno[2,3-c]pyridines as potent COT inhibitors. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4952-5. | ||||
| REF 3 | Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. | ||||
| REF 4 | Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6890-2. | ||||
| REF 5 | Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5952-6. | ||||
| REF 6 | Discovery of indazoles as inhibitors of Tpl2 kinase. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4758-61. | ||||
| REF 7 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
| REF 8 | Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor (PDGF-R) guided by water thermodynamics. J Med Chem. 2015 Jan 8;58(1):170-82. | ||||
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