Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T00176 | Target Info | |||
| Target Name | Ubiquitin-protein ligase E3 Mdm2 (MDM2) | ||||
| Synonyms |
RING-type E3 ubiquitin transferase Mdm2; P53-binding protein Mdm2; Oncoprotein Mdm2; MDM2 protein; Hdm2; E3 ubiquitin-protein ligase Mdm2; Double minute 2 protein
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| Target Type | Clinical trial Target | ||||
| Gene Name | MDM2 | ||||
| Biochemical Class | Acyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 77 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
CATECHOL
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|
Investigative | Compound Info | ||
| Synonyms |
pyrocatechol; 1,2-dihydroxybenzene; 120-80-9; 1,2-benzenediol; benzene-1,2-diol; pyrocatechin; 2-hydroxyphenol; o-Benzenediol; Pyrocatechine; o-Dihydroxybenzene; Oxyphenic acid; o-Hydroxyphenol; o-Hydroquinone; o-Dioxybenzene; o-Phenylenediol; Phthalhydroquinone; Fouramine PCH; Durafur developer C; Pelagol Grey C; benzenediol; Catechin (phenol); Fourrine 68; Benzene, o-dihydroxy-; Catechol (phenol); o-Diphenol; ortho-Hydroxyphenol; Pyrokatechol; Pyrokatechin; Katechol; ortho-Dihydroxybenzene; C.I. Oxidation Base 26
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Ethyl 6-chloro-3-[1-[(4-chlorophenyl)methyl-formylamino]-2-(cyclohexylamino)-2-oxoethyl]-1H-indole-2-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL461881; CHEMBL3950133; BDBM192163; US9187441, 8j
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| Activity |
Ki = 50000 nM
|
[2] | |||
| Compound Name |
Dimethyl 2-[[1-(4-chlorophenyl)-2,5-diphenylpyrrol-3-yl]methylidene]propanedioate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3220109
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
(+/-)-4-((1-(4-Chlorophenyl)-1-((1-(hydroxymethyl)cyclopropyl)methoxy)-3-oxoisoindolin-2-yl)methyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688292; SCHEMBL7989688; BDBM50339387
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[[4-(trifluoromethylsulfonyl)phenyl]methyl]isoindol-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688302; BDBM50339397
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
10-(4-Chlorophenyl)-9-nitropyrimido[4,5-b]quinoline-2,4-dione
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440449; BDBM50442792
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
N-[2-[7-[(2R)-Butan-2-yl]oxy-2-[4-(dimethylamino)phenyl]-6-methoxy-3-oxo-1,4-dihydroisoquinolin-1-yl]-5-chlorophenyl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2391314; CHEMBL3683102; BDBM161687; US9051279, 5
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| Activity |
IC50 = 50653.6 nM
|
[6] | |||
| Compound Name |
2-(4-Bromophenyl)-2-(5-chloro-2-oxo-3H-benzimidazol-1-yl)-N-cyclohexylacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2396756; BDBM50436043
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| Activity |
Ki = 54000 nM
|
[7] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(3-nitrobenzyl)isoindolin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688148; BDBM50339406
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| Activity |
IC50 = 54000 nM
|
[4] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione scaffold, 21
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL210545; SCHEMBL5171162; BMCL163115 Compound 12i; BDBM31289
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|
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| Activity |
IC50 = 57000 nM
|
[8] | |||
| Compound Name |
(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-5-[4-[4-[(2-methylpropan-2-yl)oxycarbonylamino]phenyl]triazol-1-yl]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3627749; BDBM50126113
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| Activity |
IC50 = 57360 nM
|
[9] | |||
| Compound Name |
Lissoclinidine B
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL461462; BDBM50273972
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| Activity |
IC50 = 58600 nM
|
[10] | |||
| Compound Name |
Isolissoclinotoxin B
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL462089; Lissoclibadin 14; BDBM50273917
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| Activity |
IC50 = 58600 nM
|
[10] | |||
| Compound Name |
Nutlin-3A
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Investigative | Compound Info | ||
| Synonyms |
Nutlin 3a; (-)-Nutlin-3; Nutlin-3a chiral; UNII-L7C92IOE65; nutlin 3; CHEMBL191334; L7C92IOE65; 548472-68-0 (4R5S, and 4S5R); Nutlin3a; C30H30Cl2N4O4; Nutlin (3a); Nutlin-3a (chiral); (4S,5R)-Nutlin-3; Nutlin-3, (-)-; cc-452; SCHEMBL1155752; HMS3649P17; Nutlin-3a, >=98% (HPLC); EX-A1359; 1960AH; 2603AH; BDBM50229787; MFCD14636430; s8059; ZINC16051336; AKOS027422740; BCP9001003; CS-0296; SB19406; NCGC00344347-05; AS-75148; HY-10029; SC-95163; A11501; W-5585; SR-01000946691; SR-01000946691-1; Q27166862; 675576-98-4 (4S5R); UNII-53IA0V845C component BDUHCSBCVGXTJM-WUFINQPMSA-N
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| Activity |
IC50 ~ 60000 nM
|
[11] | |||
| Compound Name |
2-(5-Chloro-2-oxo-3H-benzimidazol-1-yl)-N-cyclohexyl-3-phenylpropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2396747; BDBM50436041; 2-(5-Chloro-2-oxo-2,3-dihydro-1H-benzoimidazole-1-yl)-N-cyclohexyl-3-phenylpropanamide
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| Activity |
Ki ~ 60000 nM
|
[7] | |||
| Compound Name |
2-(5-Chloro-2-oxo-3H-benzimidazol-1-yl)-3-phenyl-N-(2-phenylethyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2396746; BDBM50436042
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| Activity |
Ki = 60000 nM
|
[7] | |||
| Compound Name |
6-Chloro-3-[1-[(4-chlorophenyl)methyl]-3-phenylindol-2-yl]-N-(2-morpholin-4-ylethyl)-1H-indole-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735043; BDBM50499317
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| Activity |
Ki ~ 60000 nM
|
[12] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione antagonist, 17
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL377524; BDBM31332
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| Activity |
IC50 = 60000 nM
|
[13] | |||
| Compound Name |
(3S,4S)-3-(4-Chlorophenyl)-2-[(4-chlorophenyl)methyl]-1-oxo-3,4-dihydroisoquinoline-4-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2054556; CHEMBL3219399
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| Activity |
IC50 ~ 60000 nM
|
[11] | |||
| Compound Name |
(3S,4S)-3-(4-Chlorophenyl)-2-[(4-chlorophenyl)methyl]-N-(2-methoxyethyl)-1-oxo-3,4-dihydroisoquinoline-4-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2054562; CHEMBL3219400
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| Activity |
IC50 = 62500 nM
|
[11] | |||
| Compound Name |
N-Acylpolyamine (NAPA) scaffold, 3
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL593921; BDBM35056
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| Activity |
IC50 = 63000 nM
|
[14] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione antagonist, 22
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL207845; SCHEMBL5173245; BDBM31337
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| Activity |
IC50 = 67000 nM
|
[13] | |||
| Compound Name |
5-{(3S)-3-(4-Chlorophenyl)-4-[(R)-1-(4-chlorophenyl)-ethyl]-7-iodo-2,5-dioxo-2,3,4,5-tetrahydro-benzo[e][1,4]diazepin-1-yl}-pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL210151; SCHEMBL5171589; BMCL163310 Compound 19; BDBM31305; 1,4-benzodiazepine-2,5-dione, 12b; TDP-503414; JNJ-27065844
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| Activity |
IC50 = 67000 nM
|
[13] | |||
| Compound Name |
5-[(3S)-3-(4-Chlorophenyl)-4-[1-(4-chlorophenyl)-2-methoxy-2-oxoethyl]-7-iodo-2,5-dioxo-3H-1,4-benzodiazepin-1-yl]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL210409
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| Activity |
IC50 = 67000 nM
|
[13] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-propylisoindolin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688136; SCHEMBL1826342; SCHEMBL4907072; BDBM50339418; 3-(4-chlorophenyl)-3-hydroxy-2-propylisoindol-1-one; 2-Propyl-3-hydroxy-3-(4-chlorophenyl)isoindoline-1-one
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| Activity |
IC50 = 69000 nM
|
[4] | |||
| Compound Name |
5-[(3S)-3-(4-Chlorophenyl)-4-[(1R)-1-(4-chlorophenyl)ethyl]-7-ethynyl-2,5-dioxo-3H-1,4-benzodiazepin-1-yl]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
TDP-521252; CHEMBL380214; SCHEMBL5150279; BDBM31338; JNJ-27065909; 1,4-benzodiazepine-2,5-dione antagonist, 23
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| Activity |
IC50 = 69000 nM
|
[13] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione antagonist, 2
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL379656; BDBM31318
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| Activity |
IC50 = 70000 nM
|
[13] | |||
| Compound Name |
2-[7-[(2R)-Butan-2-yl]oxy-2-[4-(dimethylamino)phenyl]-6-methoxy-3-oxo-1,4-dihydroisoquinolin-1-yl]-5-chlorobenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2395858; CHEMBL3683104; BDBM161689; US9051279, 7
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| Activity |
IC50 = 70257.7 nM
|
[6] | |||
| Compound Name |
1-[2-[7-[(2R)-Butan-2-yl]oxy-2-[4-(dimethylamino)phenyl]-6-methoxy-3-oxo-1,4-dihydroisoquinolin-1-yl]-5-chlorophenyl]-3-methylurea
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2389169; CHEMBL3683101; BDBM161686; US9051279, 4
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| Activity |
IC50 = 71187.8 nM
|
[6] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-benzylisoindolin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688137; 2-benzyl-3-(4-chlorophenyl)-3-hydroxy-2,3-dihydroisoindolin-1-one; SCHEMBL1819888; SCHEMBL1827220; BDBM50339417; AKOS024351265; MCULE-8404590411; ST50975893
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| Activity |
IC50 = 74000 nM
|
[4] | |||
| Compound Name |
10-(4-Chlorophenyl)-7-nitropyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL239274; 10-(4-chlorophenyl)-7-nitropyrimido[4,5-b]quinoline-2,4(3H,10H)-dione; Oprea1_230078; Oprea1_782832; HLI-98D; SCHEMBL3204200; DTXSID20360456; ZINC848936; BDBM50442793; NSC729132; STK711990; AKOS001620852; MCULE-2799984604; NSC-729132; ST060603; BB 0262710; EU-0071888; SR-01000436304; SR-01000436304-1; 10-(4-chlorophenyl)-7-nitro-pyrimido[4,5-b]quinoline-2,4-dione; 10-(4-chlorophenyl)-7-nitro-3,10-dihydropyrimidino[4,5-b]quinoline-2,4-dione; Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione, 10-(4-chlorophenyl)-7-nitro-
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| Activity |
IC50 ~ 75000 nM
|
[5] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione scaffold, 2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL377614; BMCL163115 Compound 12a; BDBM31288
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| Activity |
IC50 = 80000 nM
|
[8] | |||
| Compound Name |
N-Acylpolyamine (NAPA) scaffold, 2
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL611023; BDBM35055
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| Activity |
IC50 = 85000 nM
|
[14] | |||
| Compound Name |
3-Hydroxy-2-(4-nitrobenzyl)-3-phenyl-2,3-dihydroisoindol-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688144; SCHEMBL1822510; BDBM111565; BDBM50339410; US8618158, NCL-00016655; 3-hydroxy-2-[(4-nitrophenyl)methyl]-3-phenylisoindol-1-one
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| Activity |
IC50 = 87000 nM
|
[15] | |||
| Compound Name |
CID 51350115
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688161; SCHEMBL2459937; BDBM111558; US8618158, NCL-00016045; 2-[(4-acetylphenyl)methyl]-3-(4-chlorophenyl)-3-hydroxyisoindol-1-one
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| Activity |
IC50 = 88000 nM
|
[4] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione antagonist, 5
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL426321; BDBM31321
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| Activity |
IC50 = 90000 nM
|
[13] | |||
| Compound Name |
Chembl4203765
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Investigative | Compound Info | ||
| Synonyms |
BDBM50453706
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| Activity |
Ki = 93000 nM
|
[16] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-naphthalen-1-ylmethyl-2,3-dihydroisoindol-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688152; SCHEMBL2457547; BDBM111561; BDBM50339402; US8618158, NCL-00016046; 3-(4-chlorophenyl)-3-hydroxy-2-(naphthalen-1-ylmethyl)isoindol-1-one
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| Activity |
IC50 = 96000 nM
|
[15] | |||
| Compound Name |
7-Chloro-10-(2-fluorophenyl)pyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443388; BDBM50442802
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
10-(4-Chlorophenyl)-8-methylpyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443384; BDBM50442797
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
Methyl 2-(4-chlorophenyl)-2-[3-(4-chlorophenyl)-7,8-difluoro-5-oxo-2-sulfanylidene-1,3-dihydro-1,4-benzodiazepin-4-yl]acetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2089153; BDBM50420264
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| Activity |
Ki ~ 100000 nM
|
[17] | |||
| Compound Name |
4-((1-(4-Chlorophenyl)-1-hydroxy-3-oxoisoindolin-2-yl)methyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688160; BDBM50339425
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
Methyl 2-[9-chloro-3-(4-chlorophenyl)-5-oxo-2-sulfanylidene-1,3-dihydro-1,4-benzodiazepin-4-yl]-2-(4-chlorophenyl)acetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2089150; BDBM50420261
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| Activity |
Ki ~ 100000 nM
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[17] | |||
| Compound Name |
5-[[6-Amino-1-[[(2S)-1-[(3-amino-3-oxopropyl)-[5-(4-fluorophenyl)pentyl]amino]-4-carboxybutan-2-yl]-[4-(4-bromophenyl)butyl]amino]hexan-2-yl]-(2-spiro[5.5]undecan-3-ylethyl)amino]-4-(4-methylpentanoylamino)pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL594148
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
9-Chloro-10-(3-fluorophenyl)pyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443385; BDBM50442798; ZINC96286462
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
US9079913, MI-743B
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL6874794; CHEMBL3663843; BDBM170360
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| Activity |
IC50 ~ 100000 nM
|
[18] | |||
| Compound Name |
N-Acylpolyamine (NAPA) scaffold, 12
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL611334; BDBM35065
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| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
3-Benzoyl-2-(4-bromophenyl)-4-propan-2-yloxy-1-[[2-propan-2-yloxy-4-(trifluoromethyl)phenyl]methyl]-2H-pyrrol-5-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3290669; BDBM50018535
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| Activity |
Ki ~ 100000 nM
|
[19] | |||
| Compound Name |
2-[(4-Benzoylphenyl)methyl]-3-(4-chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]isoindol-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688294; SCHEMBL2459432; SCHEMBL12305427; BDBM50339389
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
9-Bromo-10-phenylpyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443383; BDBM50442796
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(4-(methylsulfonyl)benzyl)isoindolin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688156; BDBM50339421
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Chloro-10-(4-chlorophenyl)pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL224408; ZINC2255438; BDBM50442801; STK711996; AKOS005523136; MCULE-8473213363
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione,9-chloro-10-phenyl-
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420495; BDBM50438877
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
9-Chloro-10-(3-chlorophenyl)pyrimido[4,5-b]quinoline-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443386; BDBM50442799; ZINC96286463
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
4-((1-(4-Chlorophenyl)-1-hydroxy-3-oxoisoindolin-2-yl)methyl)benzenesulfonamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688157; BDBM50339422
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-(3-Bromobenzyl)-3-(4-chlorophenyl)-3-hydroxy-2,3-dihydroisoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688153; SCHEMBL2455856; BDBM50339401; 2-[(3-bromophenyl)methyl]-3-(4-chlorophenyl)-3-hydroxyisoindol-1-one
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-Benzoyl-2-(4-bromophenyl)-1-[[2-methoxy-4-(trifluoromethyl)phenyl]methyl]-4-[[(1R)-1-phenylethyl]amino]-2H-pyrrol-5-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3290679; BDBM50018548
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[19] | |||
| Compound Name |
3-Benzoyl-2-(4-bromophenyl)-1-[[2-fluoro-4-(trifluoromethyl)phenyl]methyl]-4-[[(1R)-1-phenylethyl]amino]-2H-pyrrol-5-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3290680; BDBM50018549
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[19] | |||
| Compound Name |
10-(4-Chlorophenyl)-6-(trifluoromethyl)pyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440446; BDBM50442788
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
10-Benzyl-9-(trifluoromethyl)pyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2443389; BDBM50442778
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
N-Acylpolyamine (NAPA) scaffold, 1
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL593845; BDBM35054
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[14] | |||
| Compound Name |
Methyl 2-(4-chlorophenyl)-2-[3-(4-chlorophenyl)-8-methoxy-5-oxo-2-sulfanylidene-1,3-dihydro-1,4-benzodiazepin-4-yl]acetate
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2089205; BDBM50420270
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[17] | |||
| Compound Name |
10-(2-Fluorophenyl)-9-nitropyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440450; BDBM50442794
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Methyl 2-[8-chloro-3-(4-chlorophenyl)-2-methylsulfanyl-5-oxo-3H-1,4-benzodiazepin-4-yl]-2-(4-chlorophenyl)acetate
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2089321; BDBM50420260
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[17] | |||
| Compound Name |
Methyl 2-(4-chlorophenyl)-2-[3-(4-chlorophenyl)-9-methyl-5-oxo-2-sulfanylidene-1,3-dihydro-1,4-benzodiazepin-4-yl]acetate
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2089206; BDBM50420271
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[17] | |||
| Compound Name |
3-Benzoyl-2-(4-bromophenyl)-1-[[2-fluoro-4-(trifluoromethyl)phenyl]methyl]-4-propan-2-yloxy-2H-pyrrol-5-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3290673; BDBM50018538
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[19] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(4-(methylsulfinyl)benzyl)isoindolin-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688155; BDBM50339420
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
10-(2-Fluorophenyl)-8-(trifluoromethyl)pyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440447; BDBM50442790
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
10-(4-Chlorophenyl)-8-(trifluoromethyl)pyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440445; BDBM50442786
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(4-(trifluoromethyl)benzyl)isoindolin-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688158; BDBM50339423
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
10-(4-Chlorophenyl)-7-(trifluoromethyl)pyrimido[4,5-b]quinoline-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL390761; BDBM50442787
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Ethyl 6-chloro-3-[[1-(4-chlorophenyl)tetrazol-5-yl]-(cyclohexylmethylamino)methyl]-1H-indole-2-carboxylate
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4100330; BDBM50234680
Click to Show/Hide
|
||||
| Activity |
Ki = 117000 nM
|
[20] | |||
| Compound Name |
N,N-Dimethyl-5-methylvaracin
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL462090; BDBM50273918
Click to Show/Hide
|
||||
| Activity |
IC50 = 120800 nM
|
[10] | |||
| Compound Name |
(4-Chlorophenyl)[3-(4-chlorophenyl)-7-iodo-2,5-dioxo-1,2,3,5-tetrahydro-4H-1,4-benzodiazepin-4-YL]acetic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL361103; DI-CHLORO-BENZO-DIAZEPINE; benzodiazepinedione, 1; BMCL163310 Compound 1; SCHEMBL17896492; BDBM31285; TDP-222669; JNJ-38732382; Q27459367
Click to Show/Hide
|
||||
| Activity |
IC50 = 128000 nM
|
[13] | |||
| Compound Name |
1,4-Benzodiazepine-2,5-dione antagonist, 18
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL207505; BDBM31333
Click to Show/Hide
|
||||
| Activity |
IC50 = 128000 nM
|
[13] | |||
| Compound Name |
5-[4-[Carboxy-(4-chlorophenyl)methyl]-3-(4-chlorophenyl)-7-iodo-2,5-dioxo-3H-1,4-benzodiazepin-1-yl]pentanoic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL209169; SCHEMBL4700731
Click to Show/Hide
|
||||
| Activity |
IC50 = 128000 nM
|
[13] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[(4-methylsulfanylphenyl)methyl]isoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688289; BDBM50339384
Click to Show/Hide
|
||||
| Activity |
IC50 = 175000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 11 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-((1-(4-Chlorophenyl)-1-hydroxy-3-oxoisoindolin-2-yl)methyl)pyridine 1-oxide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688167; BDBM50339432
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
2-((1-(4-Chlorophenyl)-1-hydroxy-3-oxoisoindolin-2-yl)methyl)pyridine-1-oxide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688168; BDBM50339433
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(pyridin-3-ylmethyl)isoindolin-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688164; BDBM50339429
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[(1-oxidopyridin-1-ium-4-yl)methyl]isoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688298; BDBM50339393
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
4-((1-(4-Chlorophenyl)-1-hydroxy-3-oxoisoindolin-2-yl)methyl)pyridine-1-oxide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688166; BDBM50339431
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-hydroxy-2-(pyridin-2-ylmethyl)isoindolin-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688165; BDBM50339430
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[(1-oxidopyridin-1-ium-3-yl)methyl]isoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688299; BDBM50339394
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[4] | |||
| Compound Name |
(3S,6S,9S,12S,15S,18S)-3-Benzyl-6-sec-butyl-15,18-bis(4-hydroxybenzyl)-12-isopropyl-9-methyl-1,4,7,10,13,16-hexaazacyclooctadecane-2,5,8,11,14,17-hexaone
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1256049; BDBM50327213
Click to Show/Hide
|
||||
| Activity |
IC50 = 209000 nM
|
[21] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methyl]isoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688288; BDBM50339383
Click to Show/Hide
|
||||
| Activity |
IC50 = 214000 nM
|
[4] | |||
| Compound Name |
3-(4-Chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-(pyridin-4-ylmethyl)isoindol-1-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1688295; BDBM50339390
Click to Show/Hide
|
||||
| Activity |
IC50 = 252000 nM
|
[4] | |||
| Compound Name |
Varacin
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL151233; 6-Benzopentathiepinethanamine, 8,9-dimethoxy-; Varacine; barazi n; DTXSID10158465; BDBM50240848; Q3034003; 1,2,3,4,5-Benzopentathiepin-6-ethanamine, 8,9-dimethoxy-; 2-(3,4-Dimethoxy-5,6,7,8,9-pentathia-benzocyclohepten-1-yl)-ethylamine
Click to Show/Hide
|
||||
| Activity |
IC50 > 295000 nM
|
[10] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Investigation of the inhibitory mechanism of apomorphine against MDM2-p53 interaction. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2571-2574. | ||||
| REF 2 | US patent application no. 9187441B2, p53-Mdm2 antagonists | ||||
| REF 3 | Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2-p53 and MDMX-p53 protein-protein interactionsElectronic supplementary information (ESI) available: Experimental details for compound synthesis, analytical data for all compounds and intermediates. Details for the biological evaluation. Further details for the modeling. Table of combustion analysis data. See DOI: 10.1039/c3md00161jClick here for additional data file. Medchemcomm. 2013 Sep 21;4(9):1297-1304. | ||||
| REF 4 | Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency. J Med Chem. 2011 Mar 10;54(5):1233-43. | ||||
| REF 5 | 5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2. Bioorg Med Chem. 2013 Nov 15;21(22):6868-77. | ||||
| REF 6 | US patent application no. 9051279B2, Substituted isoquinolinones and quinazolinones | ||||
| REF 7 | Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2. Bioorg Med Chem. 2013 Jul 15;21(14):3982-95. | ||||
| REF 8 | Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3115-20. | ||||
| REF 9 | Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4878-4880. | ||||
| REF 10 | Discovery of new pyridoacridine alkaloids from Lissoclinum cf. badium that inhibit the ubiquitin ligase activity of Hdm2 and stabilize p53. Bioorg Med Chem. 2008 Dec 1;16(23):10022-8. | ||||
| REF 11 | Recent applications of multicomponent reactions in medicinal chemistry. Medchemcomm. 2012;3:1189-218. | ||||
| REF 12 | 2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5661-6. | ||||
| REF 13 | Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3310-4. | ||||
| REF 14 | N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. Bioorg Med Chem. 2009 Dec 1;17(23):7884-93. | ||||
| REF 15 | US patent application no. 8618158B2, Therapeutic agents | ||||
| REF 16 | Isolation of a peptide containing d-amino acid residues that inhibits the alpha-helix-mediated p53-MDM2 interaction from a one-bead one-compound library. Bioorg Med Chem Lett. 2018 Feb 1;28(3):231-234. | ||||
| REF 17 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. Eur J Med Chem. 2012 Oct;56:10-6. | ||||
| REF 18 | US patent application no. 9079913B2, Spiro-oxindole MDM2 antagonists | ||||
| REF 19 | Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2648-50. | ||||
| REF 20 | Rational design and synthesis of 1,5-disubstituted tetrazoles as potent inhibitors of the MDM2-p53 interaction. Eur J Med Chem. 2017 Jan 27;126:384-407. | ||||
| REF 21 | Functional profiling of p53-binding sites in Hdm2 and Hdmx using a genetic selection system. Bioorg Med Chem. 2010 Aug 15;18(16):6099-108. | ||||
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