Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T17036 | Target Info | |||
| Target Name | Lysine-specific demethylase 4E (KDM4E) | ||||
| Synonyms |
Lysine-specific demethylase 4D-like; KDM4DL; KDM4D-like protein
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| Target Type | Patented-recorded Target | ||||
| Gene Name | KDM4E | ||||
| Biochemical Class | Paired donor oxygen oxidoreductase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 40 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-(carboxymethylamino)-2-oxoacetic acid
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Investigative | Compound Info | ||
| Synonyms |
N-Oxalylglycine; 5262-39-5; Oxalylglycine; Oxaloglycine; 2-((Carboxymethyl)amino)-2-oxoacetic acid; UNII-VVW38EB8YS; N-(carboxycarbonyl)glycine; N-OXALYOLGLYCINE; VVW38EB8YS; 2-oxo-3-azaglutaric acid; CHEMBL90852; Glycine, N-(carboxycarbonyl)-; CHEBI:44482; OGA; C4H5NO5; 4idz; 4nrp; 2xml; 3hqr; N-oxalyl glycine, 1a; 2oq6; 1h2k; AC1MIVD0; Glycine,N-(carboxycarbonyl)-; SCHEMBL435820; BDBM26106; CTK8F0807; DTXSID20200601; MolPort-000-141-021; ZINC1534133; N-Oxalylglycine, > 4958AE
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
daminozide
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Investigative | Compound Info | ||
| Synonyms |
DMASA; SADH; B 995; Alar; Kylar; B-NINE
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[1-(1-Benzoylazetidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621868; BDBM50498676
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| Activity |
IC50 = 50118.72 nM
|
[1] | |||
| Compound Name |
Potassium;2-[1-(3-methylphenyl)triazol-4-yl]pyridine-4-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621855; BDBM50498681
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| Activity |
IC50 = 50118.72 nM
|
[1] | |||
| Compound Name |
Potassium;2-(1-ethyltriazol-4-yl)pyridine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621854; BDBM50498691
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| Activity |
IC50 = 79432.82 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Butanoylazetidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621867; BDBM50498664
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| Activity |
IC50 = 79432.82 nM
|
[1] | |||
| Compound Name |
Potassium;2-(1-methyltriazol-4-yl)pyridine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621853; BDBM50498690
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| Activity |
IC50 = 79432.82 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Butanoylpyrrolidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621871; BDBM50498678
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-((Dimethylamino)oxy)-4-oxobutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164249; SCHEMBL19974039; BDBM50395080
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[1-[(3S)-1-Benzoylpiperidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621882; BDBM50498663; 2-[1-(1-Benzoylpiperidine-3beta-yl)-1H-1,2,3-triazole-4-yl]pyridine-4-carboxylic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Acetylpiperidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621875; BDBM50498671
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(2-Phenylethyl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621857; BDBM50498689
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
Potassium;2-(1-benzyltriazol-4-yl)pyridine-4-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621856; BDBM50498672
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[1-(3-Phenylpropanoyl)piperidin-4-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621864; BDBM50498685
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Benzoylpiperidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621878; BDBM50498680
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Ethoxycarbonylpiperidin-4-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621859; BDBM50498669
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[1-(2-Phenylacetyl)pyrrolidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621873; BDBM50498683
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Butanoylpiperidin-4-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621861; BDBM50498692
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-(Isopropylamino)-4-oxobutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164248; N-isopropylsuccinamic acid; 3-(propan-2-ylcarbamoyl)propanoic acid; NSC56468; 4-oxo-4-(propan-2-ylamino)butanoic acid; Butanoic acid, 4-[(1-methylethyl)amino]-4-oxo-; SCHEMBL94233; CTK2F3983; DTXSID20288540; ALBB-033190; ZINC1687428; BDBM50395081; MFCD02675045; NSC-56468; AKOS002675066; 4-Oxo-4-(isopropylamino)butanoic acid; MCULE-6515821068
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[(2-Furylmethyl)amino]nicotinic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774615; 2-((Furan-2-ylmethyl)amino)nicotinic acid; CTK7I9832; BDBM50153320; ZINC19770003; AKOS000213891
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-[1-(1-Propanoylazetidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621866; BDBM50498670
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-(1-Benzylpyrazol-4-yl)oxy-3H-pyrido[2,3-d]pyrimidin-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3770732; SCHEMBL16082706; BDBM50149911
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|
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(3-Carboxypropanoylamino)-trimethylazanium
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164244; BDBM50395079
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[1-[1-(2-Phenylacetyl)piperidin-4-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621863; BDBM50498686
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[1-(3-Phenylpropanoyl)piperidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621880; BDBM50498667
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|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[(3R)-1-Benzoylpiperidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621881; BDBM50498675; 2-[1-(1-Benzoylpiperidine-3alpha-yl)-1H-1,2,3-triazole-4-yl]pyridine-4-carboxylic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Propanoylpiperidin-4-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621860; BDBM50498668
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N'1,N'1,N'4,N'4-Tetramethylsuccinohydrazide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164250; SCHEMBL584428; Succinic acid dimethyl hydrazide; BDBM50395077; AKOS002685593; MCULE-9315956570
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[1-[1-(2-Phenylacetyl)azetidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621869; BDBM50498693
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[1-(2-Phenylacetyl)piperidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621879; BDBM50498679
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-[1-(3-Phenylpropanoyl)pyrrolidin-3-yl]triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621874; BDBM50498674
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[1-(1-Butanoylpiperidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621877; BDBM50498677
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
2-[(3-Methylthiophen-2-yl)methylamino]pyridine-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774435; BDBM50153321
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-[1-(1-Propanoylpiperidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621876; BDBM50498682
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
4-[Dimethylamino(methyl)amino]-4-oxobutanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164247; BDBM50395082
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[1-(1-Benzoylpiperidin-4-yl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621862; BDBM50498687
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Tranylcypromine hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
trans-2-Phenylcyclopropanamine hydrochloride; trans-2-Phenylcyclopropylamine hydrochloride; (1R,2S)-2-phenyl-cyclopropylamine hydrochloride; 2-PCPA Hydrochloride; (1R,2S)-2-Phenylcyclopropanamine hydrochloride; (1R,2S)-tranylcypromine hydrochloride; (1R,2S)-2-phenylcyclopropan-1-amine hydrochloride; TRANS-2-PHENYL-CYCLOPROPYLAMINE HYDROCHLORIDE; trans-2-Phenylcyclopropylamine HCl; Tranylcypromine (2-PCPA) HCl; DSSTox_CID_27761; DSSTox_RID_82538; DSSTox_GSID_47781; Tranylcypromine HCl; SMR000875332; (2S,1R)-2-phenylcyclopropylamine, chloride; C9H11N.HCl; 2-Phenyl-Cyclopropylamine HCl; (+)-Tranylcypromine Hydrochloride; 2-PCPA; Tranylcypromine (2-PCPA) hydrochloride; trans-2-phenylcyclopropan-1-amine hydrochloride; Rel-Tranylcypromine HCl; trans-2-Phenylcyclopropylamine hydrochloride, 97%; NCGC00016598-01; SCHEMBL56351; KSC493A7B; MLS001335868; MLS002153363; D-tranylcypromine hydrochloride; Cyclopropanamine, 2-phenyl-, hydrochloride (1:1), (1R,2S)-rel-; CHEMBL1255743; DTXSID6047781; CTK3J3070; Cyclopropanamine, 2-phenyl-, hydrochloride, (1R,2S)-rel-; HMS1568D07; Tox21_110514; 8373AH; MFCD00063602; MFCD17976456; SBB003859; AKOS022185792; Tox21_110514_1; AM84681; DS-6561; NE64568; SB35126; SB36889; KS-000005F7; NCGC00016598-02; B7514; ST50406162; (trans)-2-phenylcyclopropanamine hydrochloride; (1R,2S)-2-phenylcyclopropan-1-aminium chloride; (+/-)-Trans-2-phenyl-cyclopropylamine hydrochloride; (+/-)-trans-2-Phenylcyclopropylamine hydrochloride; J-640402; J-800286; trans-(+/-)-2-phenyl-cyclopropylamine hydrochloride; trans-(+/-)-2-Phenylcyclopropylamine hydrochloride; Q27225148; UNII-7H4CZX4FYH component ZPEFMSTTZXJOTM-OULXEKPRSA-N
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-[1-(2-Phenoxyethyl)triazol-4-yl]pyridine-4-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621858; BDBM50498688
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-3-Benzylsulfanyl-2-(oxaloamino)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1797656; BDBM50346879
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| Activity |
IC50 = 200000 nM
|
[6] | |||
| Compound Name |
(2S)-3-[(2-Methoxyphenyl)methylsulfanyl]-2-(oxaloamino)propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1797657; BDBM50346880
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|
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| Activity |
IC50 = 200000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Vorinostat
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|
Approved | Compound Info | ||
| Synonyms |
NHNPODA; SAHA; SHH; Zolinza; Merck brand of Vorinostat; OCTANEDIOIC ACID HYDROXYAMIDE PHENYLAMIDE; SAHA cpd; Suberanilohydroxamic acid; Suberoylanilide hydroxamic acid; Vorinostat MSD; Vorinostat [USAN]; M344; MK0683; SKI390; WIN64652; MK-0683; SAHA, Suberoylanilide hydroxamic acid; SW-064652; Zolinza (TN); Vorinostat (JAN/USAN); N1-hydroxy-N8-phenyloctanediamide; Zolinza, MK-0683, SAHA; N'-hydroxy-N-phenyloctanediamide; N-Hydroxy-N'-phenyl octanediamide; N-Hyrdroxy-N'-phenyloctanediamide; N-hydroxy-N'-phenyloctanediamide; N-hydroxy-N'-phenyl-octane-1,8-diotic acid diamide; Vorinostat (HDAC inhibitor)
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| Activity |
IC50 = 540000 nM
|
[6] | |||
| Compound Name |
Pyridine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
Pyridine-2,4-dicarboxylic acid; 499-80-9; 2,4-PYRIDINEDICARBOXYLIC ACID; Lutidinic acid; 2,4-Lutidinic acid; UNII-AFI29F0TVL; AFI29F0TVL; CHEBI:44737; EC 207-892-2; MJIVRKPEXXHNJT-UHFFFAOYSA-N; MFCD00149413; 2,4-Pyridinedicarboxylic acid hydrate, 99+%; 2,4-Pyridinedicarboxylicacid, hydrate (1:1); 4nrq; PD2; EINECS 207-892-2; NSC 403248; PubChem16314; 4-carboxypicolinic acid; 2vd7; 4ie0; 2w2i; pyridine carboxylate, 6a; AC1Q5UFW; ACMC-1BNB9; AC1L1V1N; 2,4-Pyridine-dicarboxylate; SCHEMBL72377; cid_10365; MLS000078055; GTPL8744
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| Activity |
Ki = 914000 nM
|
[6] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. Medchemcomm. 2014 Dec 1;5(12):1879-1886. | ||||
| REF 2 | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. J Med Chem. 2012 Jul 26;55(14):6639-43. | ||||
| REF 3 | Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives. J Med Chem. 2016 Feb 25;59(4):1357-69. | ||||
| REF 4 | Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives. J Med Chem. 2016 Feb 25;59(4):1370-87. | ||||
| REF 5 | Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities. J Med Chem. 2014 Jan 9;57(1):42-55. | ||||
| REF 6 | Inhibitors of histone demethylases. Bioorg Med Chem. 2011 Jun 15;19(12):3625-36. | ||||
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