Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T23673 | Target Info | |||
| Target Name | Proto-oncogene c-RAF (c-RAF) | ||||
| Synonyms |
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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| Target Type | Clinical trial Target | ||||
| Gene Name | RAF1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
SB 239063
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Investigative | Compound Info | ||
| Synonyms |
SB 239063; 193551-21-2; SB239063; SB-239063; UNII-HII3DC8CPI; HII3DC8CPI; CHEMBL97162; trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-(2-methoxypyridimidin-4-yl)imidazole; CHEBI:90681; TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE; trans-4-[4-(4-Fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]cyclohexanol; 4-[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazol-1-yl]cyclohexan-1-ol
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
aloisine A
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Investigative | Compound Info | ||
| Synonyms |
ALOISINE A; 4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol; 496864-16-5; RP107; 6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE; CHEMBL75680; 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP-107; ALH; 4-{7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl}phenol; 1ung; SCHEMBL80147; BDBM7377; GTPL5924; AC1NS169; 4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol; CHEBI:93641; CTK8D4068; DTXSID30416115; HMS3229A14; RM-39; BCP26893; ZINC2540737; ACT06534; IN1539; HSCI1_000219; MFCD04973541; AKOS005145972; CCG-206814; DB07364; RTC-063070; AJ-39131
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
8-chloro-quinoline-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL436817; Cyanoquinoline, 11; SCHEMBL6071997; BDBM21898; CHEBI:94979; BRD-K00088062-001-01-3; 4-[(3-Chloro-4-fluorophenyl)amino]-6-[(1H-imidazole-5-ylmethyl)amino]-8-chloro-3-quinolinecarbonitrile
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| 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
|
[4] | |||
| Compound Name |
6,6-Dimethyl-8-(1-(oxetan-3-yl)piperidin-4-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1779202; SCHEMBL897210; BDBM50344664; 6,6-dimethyl-8-[1-(oxetan-3-yl)piperidin-4-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
5-(5-Methoxy-3-pyridin-4-yl-1H-pyrrolo[3,2-b]pyridin-2-yl)benzene-1,3-diol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3219063
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
4-Methyl-3-[3-(methylsulfamoylamino)anilino]-7-pyrimidin-2-yloxychromen-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264003; SCHEMBL959114; BDBM50010474
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
CID 49806721
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1823221; SCHEMBL896410; BDBM50352760; 9-ethyl-6,6-dimethyl-8-[4-(oxetan-3-yl)piperazin-1-yl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
(2S,3S)-2-((R)-4-(4-(2-Hydroxyethoxy)phenyl)-2,5-dioxoimidazolidin-1-yl)-3-phenyl-N-(4-propionylthiazol-2-yl)butanamide.
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Investigative | Compound Info | ||
| Synonyms |
RO4927350; Ro 4927350; SCHEMBL1204725; CHEMBL2396994; ZINC43203214; RO-4927350; Z-3178
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| Activity |
Ki ~ 50000 nM
|
[8] | |||
| Compound Name |
3-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]-N-(1-phenylethyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3262871; BDBM50011572
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| Activity |
IC50 ~ 50000 nM
|
[9] | |||
| Compound Name |
5-Bromo-3-(3-phenoxy-benzylidene)-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL369490; BDBM50142032
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| Activity |
IC50 ~ 50000 nM
|
[10] | |||
| Compound Name |
[4-Methyl-3-[[5-(methylsulfamoylamino)pyridin-3-yl]methyl]-2-oxochromen-7-yl] N,N-dimethylcarbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3263997; BDBM50010468
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
6-(5-Methoxy-3-pyridin-4-yl-1H-pyrrolo[3,2-b]pyridin-2-yl)naphthalen-2-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3219062
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
N-Benzyl-N-methyl-4-(phenylsulfamoyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3355482; BDBM50043416; ZINC17334508; AKOS008571954; Z31474376
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| Activity |
IC50 ~ 100000 nM
|
[11] | |||
| Compound Name |
Meridianin E
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Investigative | Compound Info | ||
| Synonyms |
3-(2-aminopyrimidin-4-yl)-7-bromo-1H-indol-4-ol; CHEMBL296682; SCHEMBL2787193; BDBM10842
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| Activity |
IC50 ~ 100000 nM
|
[12] | |||
| Compound Name |
(3S,5E)-1-Methyl-3-(pyridin-2-ylmethyl)-5-(pyridin-2-ylmethylidene)piperidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2338335; BDBM50431025
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| Activity |
IC50 ~ 100000 nM
|
[13] | |||
| Compound Name |
Tert-butyl N-[(2R)-3-methyl-1-oxo-1-[[4-[3-(trifluoromethyl)anilino]quinazolin-6-yl]amino]butan-2-yl]carbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4092491; BDBM50237567
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
1-Phenyl-3-(4-{6-[(3,4,5-trimethoxyphenyl)amino]pyrazin-2-yl}phenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL484106; SCHEMBL12857971; BDBM25569; 2,6-Disubstituted Pyrazine, 11
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| Activity |
IC50 ~ 100000 nM
|
[15] | |||
| Compound Name |
(3R,5E)-1-Methyl-3-(pyridin-2-ylmethyl)-5-(pyridin-2-ylmethylidene)piperidin-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2338334; BDBM50431026
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|
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| Activity |
IC50 ~ 100000 nM
|
[13] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4277125
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50468565
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| Activity |
IC50 > 200000 nM
|
[16] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50. | ||||
| REF 2 | Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36. | ||||
| REF 3 | Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. J Biol Chem. 2007 Nov 16;282(46):33295-304. | ||||
| REF 4 | 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 5 | 9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors. J Med Chem. 2011 Sep 22;54(18):6286-94. | ||||
| REF 6 | Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors. Medchemcomm. 2011;2:899-903. | ||||
| REF 7 | Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14. | ||||
| REF 8 | Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators. J Med Chem. 2013 Jul 11;56(13):5219-30. | ||||
| REF 9 | Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents. Eur J Med Chem. 2014 Apr 22;77:351-60. | ||||
| REF 10 | Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. | ||||
| REF 11 | Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. ACS Med Chem Lett. 2014 Aug 7;6(1):53-7 | ||||
| REF 12 | Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1703-7. | ||||
| REF 13 | Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties. J Med Chem. 2013 May 9;56(9):3456-66. | ||||
| REF 14 | Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors. Eur J Med Chem. 2017 Apr 21;130:393-405. | ||||
| REF 15 | Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold. J Med Chem. 2008 Jun 12;51(11):3261-74. | ||||
| REF 16 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF V600E inhibition. Eur J Med Chem. 2018 Jul 15;155:725-735. | ||||
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