Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T89918 | Target Info | |||
| Target Name | Glycinamide ribonucleotide formyltransferase (GART) | ||||
| Synonyms |
Trifunctional purine biosynthetic protein adenosine-3; PRGS; PGFT
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| Target Type | Clinical trial Target | ||||
| Gene Name | GART | ||||
| Biochemical Class | Carbon-nitrogen ligase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-{4-[3-(4-Amino-6-oxo-1,6-dihydro-pyrimidin-5-yl)-propylamino]-benzoylamino}-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL31027; BDBM50005739
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| Activity |
IC50 = 52000 nM
|
[1] | |||
| Compound Name |
(S)-2-{4-[2-(4-Oxo-3,4,5,6,7,8-hexahydro-pyrido[2,3-d]pyrimidin-6-yl)-ethyl]-benzoylamino}-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL88929; BDBM50281128
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| Activity |
Ki = 82100 nM
|
[2] | |||
| Compound Name |
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL157857
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| Activity |
IC50 = 85900 nM
|
[3] | |||
| Compound Name |
1,5-Dihydroimidazo[4,5-C][1,2,6]thiadiazin-4(3h)-One 2,2-Dioxide
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Investigative | Compound Info | ||
| Synonyms |
Heterocycle, 1; CHEMBL484860; BDBM22585; Q27452602; 2,2-dioxo-1,5-dihydroimidazo[4,5-c][1,2,6]thiadiazin-4-one; 1,7-Dihydroimidazo[4,5-c][1,2,6]thiadiazine-4(3H)-one 2,2-dioxide; 4-Hydroxy-1,5-dihydroimidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxide; 1H,3H,4H,7H-2$l^{6},1,3,5,7-imidazo[4,5-c][1,2,6]thiadiazine-2,2,4-trione
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-formylamino]methyl]benzoyl]amino]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL157775
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
7-(3,4-Dihydroxy-5r-Hydroxymethyltetrahydrofuran-2-Yl)-2,2-Dioxo-1,2r,3r,7-Tetrahydro-2l6-Imidazo[4,5-C][1,2,6]thiadiazin-4s-One
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Investigative | Compound Info | ||
| Synonyms |
Nucleoside, 2; CHEMBL485481; BDBM22587; Q27451652; 7-beta-D-ribofuranosyl-1,7-dihydroimidazo[4,5-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxide
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| Activity |
Ki ~ 100000 nM
|
[4] | |||
| Compound Name |
2-{4-[3-(3-Amino-5-oxo-2,5-dihydro-[1,2,4]triazin-6-yl)-2-oxo-pyrrolidin-1-yl]-benzoylamino}-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL31107; BDBM50005738
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-methylamino]methyl]benzoyl]amino]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL156551
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2,6-Diamino-5-[6-(1,3-benzoxazol-2-yl)-6-oxohexyl]pyrimidin-4(1H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL273174; CTK2A3473; DTXSID10659169; BDBM50374377; 2,6-Diamino-5-(6-(benzo[d]oxazol-2-yl)-6-oxohexyl)pyrimidin-4(1H)-one; 4(1H)-Pyrimidinone, 2,6-diamino-5-[6-(2-benzoxazolyl)-6-oxohexyl]-
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
2-{4-[(2-Amino-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-(4-fluoro-3-nitro-benzyl)-amino]-benzoylamino}-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL286459; BDBM50089572
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| Activity |
Ki ~ 100000 nM
|
[6] | |||
| Compound Name |
(2S)-2-[[4-[2-(2-Amino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl]amino]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL314116
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| Activity |
Ki = 186000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents. J Med Chem. 1992 Apr 17;35(8):1399-410. | ||||
| REF 2 | Synthesis and biological activity of 2-desamino and 4-deoxy analogs of 5,10-dideazatetrahydrofolic acid (DDATHF). Bioorg Med Chem Lett. 1993 Dec;3(12):2657-60. | ||||
| REF 3 | Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues. J Med Chem. 1991 Feb;34(2):606-10. | ||||
| REF 4 | Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase. J Biol Chem. 2007 Apr 27;282(17):13033-46. | ||||
| REF 5 | Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. | ||||
| REF 6 | Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. Bioorg Med Chem Lett. 2000 Jul 3;10(13):1471-5. | ||||
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