Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T85540 | Target Info | |||
| Target Name | Lysine-specific demethylase 5C (KDM5C) | ||||
| Synonyms |
XE169; SMCX; Protein Xe169; Protein SmcX; Jumonji/ARID domain-containing protein 1C; JARID1C; Histone demethylase JARID1C; DXS1272E
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| Target Type | Literature-reported Target | ||||
| Gene Name | KDM5C | ||||
| Biochemical Class | Paired donor oxygen oxidoreductase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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
|
[1] | |||
| Compound Name |
2-(6-Propan-2-ylpyridin-3-yl)oxy-3H-pyrido[3,4-d]pyrimidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3769511; BDBM50149924
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| Activity |
IC50 = 50118.72 nM
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[2] | |||
| Compound Name |
Tcmdc-142577
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2098433; GSK1073731A; ZINC4304974; BDBM50153089; AKOS002050492; MCULE-2325675063; F2648-0586; 4-(ethylsulfonyl)-N-(4-(pyridin-2-yl)thiazol-2-yl)benzamide; 4-(ethylsulfonyl)-N-(4-pyridin-2-yl-1,3-thiazol-2-yl)benzamide
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| Activity |
IC50 = 52800 nM
|
[3] | |||
| Compound Name |
3-{[(Furan-2-yl)methyl]amino}pyridine-4-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3775237; SCHEMBL18247811; BDBM50153318; ZINC84485360; AKOS020330651; DA-24905; FT-0742285; J3.601.418K; 3-(2-Furanylmethylamino)pyridine-4-carboxylic acid; 3-(furan-2-ylmethylamino)pyridine-4-carboxylic acid; 4-Pyridinecarboxylic acid, 3-[(2-furanylmethyl)amino]-; Z2472763062
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| Activity |
IC50 = 63095.73 nM
|
[4] | |||
| Compound Name |
3-(Methylsulfonyl)-N-(4-(pyridin-2-yl)thiazol-2-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2094865; DNDI1417643; ZINC4303567; BDBM50153068; AKOS002051167; MCULE-6985935225; F2557-0105
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| Activity |
IC50 = 71900 nM
|
[3] | |||
| Compound Name |
8-[(4-Pyridin-2-ylpiperazin-1-yl)methyl]-3H-pyrido[3,4-d]pyrimidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774688; BDBM50153119
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| Activity |
IC50 = 88000 nM
|
[3] | |||
| Compound Name |
8-[(4-Phenylpiperazin-1-yl)methyl]-3H-pyrido[3,4-d]pyrimidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3775295; BDBM50153120
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| Activity |
IC50 ~ 100000 nM
|
[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
|
[1] | |||
| 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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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| 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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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(3-Carboxypropanoylamino)-trimethylazanium
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164244; BDBM50395079
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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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| 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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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
4-[Dimethylamino(methyl)amino]-4-oxobutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164247; BDBM50395082
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| 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
|
[5] | |||
| 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
|
[6] | |||
| Compound Name |
8-(1-Methylpyrazol-3-yl)-3H-pyrido[3,4-d]pyrimidin-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3775987; BDBM50153156
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| Activity |
IC50 = 103400 nM
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[3] | |||
| Compound Name |
8-(Piperidin-1-ylmethyl)-3H-pyrido[3,4-d]pyrimidin-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774418; BDBM50153150
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|
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| Activity |
IC50 = 111000 nM
|
[3] | |||
| Compound Name |
5-Chloro-7-[benzoylamino(3-methyl-2-thienyl)methyl]-8-quinolinol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3785164; BDBM50158849
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| Activity |
IC50 = 178000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | 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 3 | 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. J Med Chem. 2016 Feb 25;59(4):1388-409. | ||||
| REF 4 | 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 5 | Recent Progress in Histone Demethylase Inhibitors. J Med Chem. 2016 Feb 25;59(4):1308-29. | ||||
| REF 6 | 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. | ||||
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