Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25956 | Target Info | |||
| Target Name | Histone acetyltransferase p300 (EP300) | ||||
| Synonyms |
p300 HAT; Protein propionyltransferase p300; P300; Histone crotonyltransferase p300; Histone butyryltransferase p300; E1Aassociated protein p300; E1A-associated protein p300
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| Target Type | Clinical trial Target | ||||
| Gene Name | EP300 | ||||
| Biochemical Class | Acyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 19 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
C646
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Investigative | Compound Info | ||
| Synonyms |
328968-36-1; CHEMBL1797936; 4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid; C24H19N3O6; 4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid; C 646; AC1LPE4V; GTPL7004; SCHEMBL12092858; QCR-235; DTXSID30361651; MolPort-002-171-380; CHEBI:132974; ZINC8780879; s7152; 2295AH; AKOS000113052; SB19338; ST020490; C646, > J-018925; BRD-K73383190-001-03-1
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| Activity |
IC50 = 51000 nM
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[1] | |||
| Compound Name |
AMI-1
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Investigative | Compound Info | ||
| Synonyms |
AMI1; AMI 1
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| Activity |
IC50 = 118500 nM
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[2] | |||
| Compound Name |
Chembl4289431
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Investigative | Compound Info | ||
| Synonyms |
BDBM50467838
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| Activity |
IC50 ~ 50000 nM
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[3] | |||
| Compound Name |
6-Hydroxy-5-[(Z)-indol-3-ylidenemethyl]-1-methyl-2-sulfanylidenepyrimidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2203537; BDBM50400735
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
(5E)-1-Methyl-5-{[5-(morpholin-4-yl)furan-2-yl]methylidene}-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4287521; ZINC4724053; BDBM50467834; STK189981; AKOS005413093
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
Chembl4170165
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Investigative | Compound Info | ||
| Synonyms |
BDBM50282492
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| Activity |
IC50 = 52000 nM
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[4] | |||
| Compound Name |
5-(1,2-Thiazol-5-yldisulfanyl)-1,2-thiazole
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Investigative | Compound Info | ||
| Synonyms |
NU 9056; CHEMBL3774630; SCHEMBL7171043; 1,2-Di(isothiazol-5-yl)disulfane; 1,2-bis(isothiazol-5-yl)disulfane; BCP17389; BDBM50151660; ZINC98052699; AKOS024458409; NU-9056;NU9056; J-008045
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| Activity |
IC50 = 58000 nM
|
[5] | |||
| Compound Name |
Chembl4170179
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Investigative | Compound Info | ||
| Synonyms |
BDBM50282628
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| Activity |
IC50 = 60000 nM
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[4] | |||
| Compound Name |
6-[(5Z)-5-[1-[(4-Methoxyphenyl)methyl]-2-oxoindol-3-ylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3221335
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| Activity |
IC50 = 61900 nM
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[6] | |||
| Compound Name |
6-{(5Z)-5-[1-(4-Methylbenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl}hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3221334; ZINC1769377; STK880889; AKOS002271537
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| Activity |
IC50 = 81000 nM
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[6] | |||
| Compound Name |
4-Methoxynaphthalen-1-amine hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
1-Amino-4-methoxynaphthalen HCl; 4-methoxynaphthalen-1-amine;hydrochloride; 1-amino-4-methoxynaphthalene hydrochloride; 4-methoxy-1-aminonaphthalene hydrochloride; F2146-0572; SCHEMBL6155452; CHEMBL4175261; CTK8B6526; DTXSID80596214; ANW-53598; MFCD16877105; AKOS015999240; MCULE-5355245253; 1-Amino-4-methoxynaphthalen hydrochloride; V9189; 1-Naphthalenamine, 4-methoxy-, hydrochloride; B-8333; 4-Methoxynaphthalen-1-amine--hydrogen chloride (1/1); Z2681942354
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| Activity |
IC50 = 95000 nM
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[4] | |||
| Compound Name |
8-[(5Z)-5-[1-[(4-Methylphenyl)methyl]-2-oxoindol-3-ylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]octanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3221338
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| Activity |
IC50 = 95300 nM
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[6] | |||
| Compound Name |
4-Nitro-1-naphthol
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Investigative | Compound Info | ||
| Synonyms |
4-nitronaphthalen-1-ol; 1-Naphthalenol, 4-nitro-; 1-Hydroxy-4-nitronaphthalene; 4-nitronaphthol; CHEMBL2312200; 4-Nitronaphthalenol; NSC400336; PubChem13796; ACMC-209mko; 4-nitro-1-naphthalenol; 4-nitro-naphthalen-1-ol; 1-Naphthalenol,4-nitro-; 4-nitro-1-hydroxynaphthalene; SCHEMBL589663; CTK5B1742; DTXSID00209238; ACN-S002712; ALBB-014693; ANW-33526; BBL101777; BDBM50425036; MFCD02179392; SBB067137; STL555574; ZINC35193837; AKOS005174640; MCULE-5007401844; NSC-400336; AC-29203; AS-13065; SC-45968; AB0012922; DB-053652; AM20040822; FT-0632516; N0672; R5601; ST50408514; A832781; F1905-7194; Z2607956390
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| Activity |
IC50 = 106000 nM
|
[4] | |||
| Compound Name |
Cyqualon
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Investigative | Compound Info | ||
| Synonyms |
Cyclovalone; Curcumoid; Cycvalon; 2,6-Divanillylidenecyclohexanone; Divanil; Divanon; Flavugal; Tsikvalon; VANILONE; Divanillalcyclohexanone; CHEMBL17205; (2E,6E)-2,6-bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone; 2,6-Divanillidenecyclohexanone; 2,6-Bis((4-hydroxy-3-methoxyphenyl)methylene)cyclohexanone; 2,6-Bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone; SMR000554641; 2,6-Bis((4-hydroxy-3-methoxyphenyl)methylene)cyclohexan-1-one; 2,6-bis[(4-hydroxy-3-methoxyphenyl)methylene]cyclohexan-1-one; NCGC00164486-01; MLS000881144; MLS000881192; MLS001194951; SCHEMBL554417; Cyclohexanone,6-vanillylidene-; Cyclohexanone,6-divanillylidene-; cid_1550234; HMS642D03; GT-18; HMS2865P11; NSC26727; ZINC4468855; BDBM50067033; NSC-26727; NSC652893; (2E,6E)-2,6-bis[(4-hydroxy-3-methoxyphenyl)methylidene]cyclohexan-1-one; AKOS001571214; NSC-652893; NCGC00164486-02; NCGC00164486-03; ST50975748; WLN: L6YVYTJ AU1R DQ CO1& CU1R DQ CO1; 2,6-Bis-(4-hydroxy-3-methoxy-benzylidene)-cyclohexanone; 2,6-Bis[(E)-3-methoxy-4-hydroxybenzylidene]cyclohexanone; Cyclohexanone,6-bis[(4-hydroxy-3-methoxyphenyl)methylene]-; 2,6-bis((3-methoxy-4-hydroxyphenyl)methylene)-cyclohexanone; (2E,6E)-2,6-bis[(4-hydroxy-3-methoxy-phenyl)methylene]cyclohexanone; 2,6-Bis-[1-(4-hydroxy-3-methoxy-phenyl)-meth-(E)-ylidene]-cyclohexanone
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| Activity |
IC50 = 111000 nM
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[7] | |||
| Compound Name |
[(3,5-Dimethyl-4-oxocyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3775671; SR-01000239221; SCHEMBL15299803; AOB4204; SYN5191; ZINC2868042; BDBM50151658; NSC764414; AKOS002262677; MCULE-3464420106; NSC 764414; L002(NSC764414); AS-16551; HY-100671; CS-0019911; L 002; ST50168582; MLS-0437249.0001; J-018664; SR-01000239221-1; SR-01000239221-3; 4-(4-methoxyphenylsulfonyloxyimino)-2,6-dimethylcyclohexa-2,5-dienone; 4-((((4-Methoxyphenyl)sulfonyl)oxy)imino)-2,6-dimethylcyclohexa-2,5-dien-1-one
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| Activity |
IC50 = 128000 nM
|
[5] | |||
| Compound Name |
2-[4-[2-[3-(3,4-Dimethoxyphenyl)-5-thiophen-2-yl-3,4-dihydropyrazol-2-yl]-1,3-thiazol-4-yl]phenyl]isoindole-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3775244; SCHEMBL13856622; BDBM50151659; MCULE-7371142363
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| Activity |
IC50 = 150000 nM
|
[5] | |||
| Compound Name |
6-[(5Z)-5-[1-[(4-Nitrophenyl)methyl]-2-oxoindol-3-ylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3221336
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| Activity |
IC50 = 151900 nM
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[6] | |||
| Compound Name |
2,6-Bis(3-carboxy-4-hydroxybenzylidene)cyclohexanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL222543; BDBM50207588
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| Activity |
IC50 = 168000 nM
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[7] | |||
| Compound Name |
Chembl4299337
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Investigative | Compound Info | ||
| Activity |
IC50 = 200000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 6 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-AMINOPHENOL
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Investigative | Compound Info | ||
| Synonyms |
4-aminophenol; 123-30-8; p-aminophenol; 4-hydroxyaniline; p-hydroxyaniline; Phenol, 4-amino-; Paranol; Certinal; Citol; Azol; 4-aminobenzenol; Fouramine P; Ursol P Base; Rodinal; p-Hydroxyphenylamine; Benzofur P; Fourrine P Base; Pelagol P Base; Tertral P Base; Ursol P; Furro P Base; Nako Brown R; Durafur Brown RB; 4-Amino-1-hydroxybenzene; Renal AC; Fourrine 84; Phenol, p-amino-; Zoba Brown P Base; 4-AMINO-PHENOL; UNAL; C.I. Oxidation Base 6; 1-Amino-4-hydroxybenzene; Pelagol Grey P Base; BASF Ursol P Base; p-Aminofenol; Para-aminophenol
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| Activity |
IC50 > 500000 nM
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[4] | |||
| Compound Name |
2,6-Bis(3,4-dihydroxybenzylidene)cyclohexanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL129148; SCHEMBL14259649; RDS-1158; ZINC5843952; (2E,6E)-2,6-bis[(3,4-dihydroxyphenyl)methylidene]cyclohexan-1-one; BDBM50067027; NSC652890; NSC-652890; 2,6-Bis-(3,4-dihydroxy-benzylidene)-cyclohexanone; 2,6-Bis((3,4-dihydroxyphenyl)methylene)cyclohexan-1-one; (2E,6E)-2,6-bis[(3,4-dihydroxyphenyl)methylene]cyclohexanone; 2,6-Bis-[1-(3,4-dihydroxy-phenyl)-meth-(E)-ylidene]-cyclohexanone
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| Activity |
IC50 = 233000 nM
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[7] | |||
| Compound Name |
6-{(5Z)-5-[1-(4-Fluorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl}hexanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3221317; ZINC1820778; STK706542; AKOS005178237
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| Activity |
IC50 = 244100 nM
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[6] | |||
| Compound Name |
Chembl4163878
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Investigative | Compound Info | ||
| Synonyms |
BDBM50282493
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| Activity |
IC50 = 250000 nM
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[4] | |||
| Compound Name |
Ctpb
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774466; n-(4-chloro-3-trifluoromethyl-phenyl)-2-ethoxy-6-pentadecyl-benzamide; N-[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]-2-ETHOXY-6-PENTADECYLBENZAMIDE; SCHEMBL998270; CTK8E7808; DTXSID20437930; BDBM50151652; ZINC100306346; HY-124960; CS-0089747; BRD-K43234716-001-01-2; Q27162396; N-[3-(Trifluoromethyl)-4-chlorophenyl]-2-ethoxy-6-pentadecylbenzamide
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| Activity |
IC50 = 275000 nM
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[5] | |||
| Compound Name |
2-Hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trienyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL455368; 2-hydroxy-6-((8Z,11Z)-pentadeca-8,11,14-trienyl)benzoic acid; 6-[8(Z),11(Z),14-pentadecatrienyl]salicylic acid; 6-{8(Z),11(Z),14-pentadecatrienyl}salicylic acid; MEGxp0_000812; SCHEMBL4142096; ACon1_001118; DTXSID70872877; 2-Pentadecyl-6-hydroxybenzoic acid; BDBM50292429; LMPK15040001; ZINC17198574; MCULE-7532607179; NCGC00169660-01; NCGC00169660-02; Q527648; (15:3)-Anacardic acid, >=85% (LC/MS-ELSD); BRD-K93380348-001-01-8; 6[8''(Z ),11''(Z ),14''-pentadecatrienyl]salicylicacid; 2-hydroxy-6-(8Z,11Z)-8,11,14-pentadecatrien-1-yl-benzoicacid; 2-Hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trien-1-yl]benzoic acid
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| Activity |
IC50 > 1000000 nM
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[8] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Characterizing the Covalent Targets of a Small Molecule Inhibitor of the Lysine Acetyltransferase P300. ACS Med Chem Lett. 2015 Oct 31;7(2):151-5. | ||||
| REF 2 | Discovery and mechanistic study of a class of protein arginine methylation inhibitors. J Med Chem. 2010 Aug 26;53(16):6028-39. | ||||
| REF 3 | Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407. | ||||
| REF 4 | The relevance of K i calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor. Eur J Med Chem. 2017 Aug 18;136:480-486. | ||||
| REF 5 | KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases. J Med Chem. 2016 Feb 25;59(4):1249-70. | ||||
| REF 6 | Rhodanine carboxylic acids as novel inhibitors of histone acetyltransferases. Medchemcomm. 2012;3:305-11. | ||||
| REF 7 | Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase. J Med Chem. 2007 Apr 19;50(8):1973-7. | ||||
| REF 8 | Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60. Bioorg Med Chem. 2009 Feb 1;17(3):1381-6. | ||||
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