Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T71949 | Target Info | |||
Target Name | Lysine-specific demethylase 2A (KDM2A) | ||||
Synonyms |
FBXL11; FBL7; F-box/LRR-repeat protein 11; F-box protein Lilina; F-box protein FBL7; F-box and leucine-rich repeat protein 11; CXXC8; CXXC-type zinc finger protein 8; [Histone-H3]-lysine-36 demethylase 1A; KIAA1004; JmjC domain-containing histone demethylation protein 1A; JHDM1A
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Target Type | Literature-reported Target | ||||
Gene Name | KDM2A | ||||
UniProt ID |
Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
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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 = 50118.72 nM
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[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 = 50118.72 nM
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[1] | |||
Compound Name |
(3-Carboxypropanoylamino)-trimethylazanium
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2164244; BDBM50395079
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Activity |
IC50 = 63000 nM
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[2] | |||
Compound Name |
2-[5-[(5-Methyl-1,2-oxazol-3-yl)carbonylamino]-2-oxidanyl-phenyl]pyridine-4-carboxylic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3775867; BDBM50151393; 6Z1
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Activity |
IC50 = 76000 nM
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[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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Activity |
IC50 = 79432.82 nM
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[1] | |||
Compound Name |
2-[5-[(4-Hydroxyphenyl)carbonylamino]-2-Oxidanyl-Phenyl]pyridine-4-Carboxylic Acid
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Investigative | Compound Info | ||
Synonyms |
KDM4C-IN-35; CHEMBL3775262; 2-[2-Hydroxy-5-(4-hydroxy-benzoylamino)-phenyl]-isonicotinic acid; BDBM50151392; J3.601.435K; 2-[2-Hydroxy-5-(4-hydroxybenzoylamino)phenyl]pyridine-4-carboxylic acid
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Activity |
IC50 = 89000 nM
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[3] | |||
Compound Name |
2-[5-[2-(3-Methoxyphenyl)ethanoylamino]-2-Oxidanyl-Phenyl]pyridine-4-Carboxylic Acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3775272; 9CJ; BDBM50151397
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Activity |
IC50 = 89000 nM
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[3] | |||
Compound Name |
2-[5-(2-Methoxyethanoylamino)-2-Oxidanyl-Phenyl]pyridine-4-Carboxylic Acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3775380; 7WH; BDBM50151399
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Activity |
IC50 = 91000 nM
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[3] | |||
Compound Name |
2-(5-Acetamido-2-Oxidanyl-Phenyl)pyridine-4-Carboxylic Acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3774598; S2X; BDBM50151401
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Activity |
IC50 ~ 100000 nM
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[3] | |||
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
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[2] | |||
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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Activity |
IC50 ~ 100000 nM
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[2] | |||
Compound Name |
5-Quinolinecarboxylic acid, 8-hydroxy-, octyl ester
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3785984; cmp5;compound 5; BDBM50158888
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Activity |
IC50 ~ 100000 nM
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[4] | |||
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
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[5] | |||
Compound Name |
2-[1-(1-Acetylazetidin-3-yl)triazol-4-yl]pyridine-4-carboxylic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3621865; BDBM50498661
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
(2R)-2-Hydroxypentanedioic acid
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Investigative | Compound Info | ||
Synonyms |
(R)-2-hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid; D-2-Hydroxyglutaric acid; (R)-Hydroxyglutarate; (R)-2-hydroxyglutarate; d-alpha-hydroxyglutaric acid; Pentanedioic acid, 2-hydroxy-, (2R)-; CHEMBL1614745; D-2-Hydroxyglutarate; Glutaric acid, 2-hydroxy-; D-Hydroxyglutarate; D-a-Hydroxyglutarate; 2-hydroxy-D-Glutarate; (R)-a-Hydroxyglutarate; delta-2-Hydroxyglutarate; D-a-Hydroxyglutaric acid; 2-hydroxy-delta-Glutarate; (2R)-hydroxyglutaric acid; 2-hydroxy-D-Glutaric acid; (R)-alpha-Hydroxyglutarate; delta-alpha-Hydroxyglutarate; SCHEMBL8032; (R)-a-Hydroxyglutaric acid; delta-2-Hydroxyglutaric acid; (R)-2-hydroxy-Pentanedioate; 2-hydroxy-delta-Glutaric acid; (R)-alpha-Hydroxyglutaric acid; delta-alpha-Hydroxyglutaric acid; (R)-2-hydroxy-Pentanedioic acid; DTXSID80897218; ZINC402968; BDBM50361471; AKOS027325193; HY-113038; CS-0059411; C01087; 93397C3E-3CE9-4FEA-A2ED-8F6FA59A1FEA; Q27104222; Z2217110365
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Activity |
IC50 = 106000 nM
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[6] | |||
Compound Name |
2-(3-Oxo-6-hydroxy-3H-xanthene-9-yl)-5-[3-[4-(aminomethyl)benzyl]-3-[4-[1,4-dioxo-4-(sodiooxy)-2-butenylhydroxyamino]butyl]thioureido]benzoic acid sodium salt
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2392184
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Activity |
IC50 = 109000 nM
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[7] | |||
Click to Show/Hide the Information of All Poor Binders |
References | Top | ||||
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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 | Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. J Med Chem. 2016 Feb 25;59(4):1580-98. | ||||
REF 4 | Recent Progress in Histone Demethylase Inhibitors. J Med Chem. 2016 Feb 25;59(4):1308-29. | ||||
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 | Lysine demethylases inhibitors. J Med Chem. 2011 Dec 22;54(24):8236-50. | ||||
REF 7 | Quantitative analysis of histone demethylase probes using fluorescence polarization. J Med Chem. 2013 Jun 27;56(12):5198-202. |
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