Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T75596 | Target Info | |||
| Target Name | Methionine aminopeptidase 2 (METAP2) | ||||
| Synonyms |
Peptidase M 2; P67eIF2; P67; MetAP 2; METAP2; Initiation factor 2 associated 67 kDa glycoprotein; (MetAP)-2
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|
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| Target Type | Clinical trial Target | ||||
| Gene Name | METAP2 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 39 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
[(3S,6S)-7-Oxo-6-[[(E,2R,3R,4S,5R)-3,4,5-trihydroxy-2-methoxy-8-methylnon-6-enoyl]amino]azepan-3-yl] 12-methyltridecanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4061080; BDBM50267195
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
[(3S,6S)-1-Methyl-7-oxo-6-[[(E,2R,3R,4S,5R)-3,4,5-trihydroxy-2-methoxy-8-methylnon-6-enoyl]amino]azepan-3-yl] 12-methyltetradecanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL539894; BDBM50295173
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(S)-2-((S)-3-Amino-4-benzylsulfanyl-2-hydroxy-butyrylamino)-propionic acid ethyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL169482; BDBM50141685
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
N'-[(2S,3R)-3-Amino-3-cyclohexyl-2-hydroxypropanoyl]naphthalene-2-carbohydrazide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL171615; BDBM50141758; Naphthalene-2-carboxylic acid N''-((S)-hydroxy-1-(R)-3-amino-3-cyclohexyl-2-oxo-propyl)-hydrazide
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
1,4-Dihydroxy-3-methoxy-2-[2-methyl-3-(3-methyl-but-2-enyl)-oxiranyl]-cyclohexanecarbaldehyde
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL325412; BDBM50131563
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|
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| Activity |
IC50 = 53600 nM
|
[4] | |||
| Compound Name |
(1S,5S)-5-(Hydroxymethyl)-1-methoxy-6-(6-methylhept-5-en-2-yl)bicyclo[3.1.0]hexan-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL214053; BDBM50194622; (1S,5S,6R)-5-(hydroxymethyl)-1-methoxy-6''-(6''-methylhept-5''-en-2''-yl)bicyclo[3.1.0]hexan-2-one
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| Activity |
IC50 = 57500 nM
|
[5] | |||
| Compound Name |
Anthranilic Acid Sulfonamide, 10ap
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL210342; SCHEMBL3981259; BDBM17520
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| Activity |
IC50 = 66000 nM
|
[6] | |||
| Compound Name |
(S)-2-((S)-3-Amino-4-cyclohexylmethylsulfanyl-2-hydroxy-butyrylamino)-propionic acid ethyl ester
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL169405; BDBM50141684
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|
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| Activity |
IC50 = 74000 nM
|
[3] | |||
| Compound Name |
(S)-2-Amino-N-hydroxy-4-methylsulfanyl-N-[(2-pyridin-2-yl-ethylcarbamoyl)-methyl]-butyramide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL164506; BDBM50137355
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|
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| Activity |
Ki = 91000 nM
|
[7] | |||
| Compound Name |
4-[4-(4-Methoxyphenyl)piperazin-1-Yl]-2-(Pyridin-2-Yl)quinazoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4079583; SCHEMBL12667691; BDBM50267199; Q27460483; 2-(2-Pyridinyl)-4-[4-(4-methoxyphenyl)piperazino]quinazoline
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S,3R)-3-Amino-4-cyclohexyl-N-((S)-1,2-dimethyl-propyl)-2-hydroxy-butyramide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL167481; BDBM50141732
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Phenethyl-(2-pyridin-2-yl-quinazolin-4-yl)-amine
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|
Investigative | Compound Info | ||
| Synonyms |
MLS000769840; SMR000434573; N-(2-phenylethyl)-2-pyridin-2-ylquinazolin-4-amine; cid_937982; SCHEMBL2905797; CHEMBL1518085; BDBM47468; ZINC532702; STK558250; AKOS005483971; MCULE-2107436054; phenethyl-[2-(2-pyridyl)quinazolin-4-yl]amine; SR-01000766277; SR-01000766277-2; N-(2-phenylethyl)-2-(2-pyridinyl)-4-quinazolinamine; N-(2-phenylethyl)-2-pyridin-2-yl-quinazolin-4-amine; N-(2-phenylethyl)-2-(pyridin-2-yl)quinazolin-4-amine
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-[(2S)-1-Oxo-3-phenyl-1-[4-(2-pyridin-2-ylquinolin-4-yl)piperazin-1-yl]propan-2-yl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375609; BDBM50433373
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(2-Pyridin-2-ylquinolin-4-yl)piperazin-1-yl]benzaldehyde
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375622; BDBM50433393
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(4-Nitrophenyl)piperazin-1-yl]-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375621; BDBM50433392
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5,6-Disubstituted anthranilic acid sulfonamide, 9l
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL388246; BDBM17620; 6-[(2-bromo-4-fluorobenzene)sulfonamido]-3-(1H-imidazol-4-yl)-2-methoxybenzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
4-[4-(3,4-Dichlorophenyl)piperazin-1-yl]-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375607; BDBM50433398
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5,6-Disubstituted anthranilic acid sulfonamide, 9k
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL230384; BDBM17619; 6-[(2-bromo-4-fluorobenzene)sulfonamido]-3-(furan-2-yl)-2-methoxybenzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
2-[4-[4-(2-Pyridin-2-ylquinolin-4-yl)piperazin-1-yl]phenoxy]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375619; BDBM50433390
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(4-Methylphenyl)sulfonylpiperazin-1-yl]-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375608; BDBM50433399
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(4-Methoxyphenyl)piperazin-1-yl]-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375624; BDBM50433395
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(2-Pyridin-2-ylquinolin-4-yl)piperazin-1-yl]phenol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375620; BDBM50433391
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
N-[5-[2-Oxo-2-[4-(2-pyridin-2-ylquinolin-4-yl)piperazin-1-yl]ethyl]-1,3-thiazol-2-yl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375610; BDBM50433374
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
2-(benzo[c][1,2,5]thiadiazole-4-sulfonamido)-5-bromobenzoic acid; sulfonamide compound, 2; ChemDiv1_000019; Oprea1_626691; Oprea1_776953; CBDivE_004835; MLS001209579; CHEMBL378442; SCHEMBL7820192; BDBM17596; HMS587A19; HMS2841P15; ZINC715914; 2-(2,1,3-benzothiadiazol-4-ylsulfonylamino)-5-bromobenzoic acid; 2-(Benzo[1,2,5]thiadiazole-4-sulfonylamino)-5-bromo-benzoic acid; STK751176; AKOS000538927; MCULE-4876792961; SMR000513426; ST50222795; SR-01000388966; SR-01000388966-1; F0266-0134; 2-(2,1,3-benzothiadiazole-4-sulfonamido)-5-bromobenzoic acid; 2-[(benzo[2,3-c]1,2,5-thiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[10] | |||
| Compound Name |
4-(Morpholin-4-yl)-2-(pyridin-2-yl)quinazoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1329554; MLS000040058; HMS2323L16; ZINC521854; BDBM50433382; STK553207; AKOS030521447; MCULE-4052192741; SMR000042589
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
1-[4-[4-(2-Pyridin-2-ylquinolin-4-yl)piperazin-1-yl]phenyl]ethanol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375615; BDBM50433386
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Ethyl 2-[4-[4-(2-pyridin-2-ylquinolin-4-yl)piperazin-1-yl]phenoxy]acetate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375618; BDBM50433389
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5,6-Disubstituted anthranilic acid sulfonamide, 9g
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL230279; SCHEMBL3987788; BDBM17615; 6-[(4-fluorobenzene)sulfonamido]-3-(1-hydroxyethyl)-2-methylbenzoic acid; 6-[(4-fluorophenyl)sulfonylamino]-3-(1-hydroxyethyl)-2-methylbenzoic acid; 6-{[(4-fluorophenyl)sulfonyl]amino}-3-[1-hydroxyethyl]-2-methylbenzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
4-(4-Methylpiperazino)-2-(2-pyridyl)quinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL49678; DTXSID70332365; BDBM50433385; ZINC19908879; MCULE-7478533139; 4-(4-methylpiperazin-1-yl)-2-(2-pyridyl)quinoline; 4-(4-Methyl-1-piperazinyl)-2-(2-pyridinyl)quinoline; N-(4-Methyl-1-piperazinyl)-2-(2-pyridinyl)quinoline; Quinoline, 4-(4-methyl-1-piperazinyl)-2-(2-pyridinyl)-, dihydrobromide
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(2-Pyridin-2-ylquinolin-4-yl)piperazin-1-yl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375617; BDBM50433388
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-[4-(4-Prop-2-enoxyphenyl)piperazin-1-yl]-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375623; BDBM50433394
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-Chloro-2-(pyridin-2-yl)quinazoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375629; Quinazoline, 4-chloro-2-(2-pyridinyl)-; 4-chloro-2-pyridin-2-ylquinazoline; ACMC-20luwb; C13H8ClN3; SCHEMBL4473954; CTK3I0435; DTXSID20359002; ZINC522072; 2-(2-Pyridyl)-4-chloroquinazoline; BDBM50433378; STK549316; 4-chloro-2(yridin-2-yl) quinazoline; AKOS005232589; MCULE-2945868860; NE51246; Z1982491203
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Ethyl 4-[4-(2-pyridin-2-ylquinolin-4-yl)piperazin-1-yl]benzoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375616; BDBM50433387
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5,6-Disubstituted anthranilic acid sulfonamide, 9f
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL388034; SCHEMBL3981126; BDBM17614; 6-[(4-fluorobenzene)sulfonamido]-3-(hydroxymethyl)-2-methylbenzoic acid; 6-[(4-fluorophenyl)sulfonylamino]-3-(hydroxymethyl)-2-methylbenzoic acid; 6-{[(4-fluorophenyl)sulfonyl]amino}-3-(hydroxymethyl)-2-methylbenzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
4-Piperidin-1-yl-2-pyridin-2-ylquinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375614; MMV560185; Maybridge3_003438; Oprea1_797237; SCHEMBL2547815; HMS1440M06; BDBM50433383; CCG-48252; ZINC20432400; AKOS024326127; MCULE-2929383612; IDI1_014825; 4-PIPERIDIN-1-YL-2-PYRIDIN-2-YL-QUINOLINE; SR-01000637808-1
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Quinoline, 4-(4-morpholinyl)-2-(2-pyridinyl)-
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|
Investigative | Compound Info | ||
| Synonyms |
4-Morpholino-2-(2-pyridyl)quinoline; 4-(4-MORPHOLINYL)-2-(PYRIDIN-2-YL)QUINOLINE; CHEMBL45721; 4-(2-(Pyridin-2-yl)quinolin-4-yl)morpholine; 4-(2-pyridin-2-ylquinolin-4-yl)morpholine; SCHEMBL2545683; CTK4B8765; DTXSID20158335; BDBM50433384; GEO-03297; ZINC19809797; 4-Morpholino-2-(2-pyridinyl)quinoline; MCULE-6426149545; 4-[2-(2-pyridyl)-4-quinolyl]morpholine
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|
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
4-(Piperidin-1-yl)-2-(pyridin-2-yl)quinazoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375613; ZINC529784; BDBM50433381; STK556611; AKOS005482756; MCULE-8182680769; NCGC00274371-01; AB01278587-01
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| Activity |
EC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5,6-Disubstituted anthranilic acid sulfonamide, 17b
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL230493; SCHEMBL3984544; BDBM17626; 2-(carboxymethoxy)-3-ethyl-6-[(4-fluorobenzene)sulfonamido]benzoic acid; 2-(carboxymethoxy)-3-ethyl-6-[(4-fluorophenyl)sulfonylamino]benzoic acid
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
(S)-2-Amino-hexanoic acid hydroxy-[(2-pyridin-2-yl-ethylcarbamoyl)-methyl]-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL167633; BDBM50137352
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| Activity |
Ki = 164000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 7 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-(5-Chloropyridin-2-yl)-4-[4-(4-methoxyphenyl)piperazin-1-yl]quinoline
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375625; BDBM50433396
Click to Show/Hide
|
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| Activity |
EC50 > 200000 nM
|
[8] | |||
| Compound Name |
2-(5-Bromopyridin-2-yl)-4-[4-(4-methoxyphenyl)piperazin-1-yl]quinoline
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375626; BDBM50433397
Click to Show/Hide
|
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| Activity |
EC50 > 200000 nM
|
[8] | |||
| Compound Name |
Tert-Butyl {2-[(1,3-Thiazol-2-Ylamino)carbonyl]pyridin-3-Yl}carbamate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL327579; BDBM17847; DB07902; pyridine-2-carboxylic acid inhibitor, 1; Q27097137; tert-butyl [2-(1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate; tert-butyl N-[2-(1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate; N-(2-Thiazolyl)-3-[(tert-butoxycarbonyl)amino]-2-pyridinecarboxamide
Click to Show/Hide
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| Activity |
IC50 > 300000 nM
|
[1] | |||
| Compound Name |
N-[2-(2H-Isoindol-1-yl)ethyl]-2-pyridin-2-ylquinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375612; BDBM50433380
Click to Show/Hide
|
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| Activity |
EC50 > 300000 nM
|
[8] | |||
| Compound Name |
N-Phenyl-N'-(2-pyridin-2-ylquinazolin-4-yl)ethane-1,2-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2375611; SCHEMBL12674275; BDBM50433379
Click to Show/Hide
|
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| Activity |
EC50 > 300000 nM
|
[8] | |||
| Compound Name |
[((R)-2-Amino-propionyl)-hydroxy-amino]-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL164406; D-Ala-N-Hydroxy-Gly-OH; BDBM50137354
Click to Show/Hide
|
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| Activity |
Ki = 600000 nM
|
[7] | |||
| Compound Name |
[((S)-2-Amino-4-methylsulfanyl-butyryl)-hydroxy-amino]-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL349154; L-Met-N-Hydroxy-Gly-OH; BDBM50137353
Click to Show/Hide
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| Activity |
Ki = 1300000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The Bengamides: A Mini-Review of Natural Sources, Analogues, Biological Properties, Biosynthetic Origins, and Future Prospects. J Nat Prod. 2017 Mar 24;80(3):740-755. | ||||
| REF 2 | A selective account of effective paradigms and significant outcomes in the discovery of inspirational marine natural products. J Nat Prod. 2009 Mar 27;72(3):588-603. | ||||
| REF 3 | 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2. Bioorg Med Chem Lett. 2004 Feb 23;14(4):865-8. | ||||
| REF 4 | Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis. J Med Chem. 2003 Jul 31;46(16):3452-4. | ||||
| REF 5 | Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo. J Med Chem. 2006 Sep 21;49(19):5645-8. | ||||
| REF 6 | Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of a... J Med Chem. 2006 Jun 29;49(13):3832-49. | ||||
| REF 7 | Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors. Bioorg Med Chem Lett. 2004 Jan 5;14(1):77-9. | ||||
| REF 8 | Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells. J Med Chem. 2013 May 23;56(10):3996-4016. | ||||
| REF 9 | Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids. Bioorg Med Chem Lett. 2007 May 15;17(10):2817-22. | ||||
| REF 10 | Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. | ||||
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