Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T69912 | Target Info | |||
| Target Name | Platelet-activating factor acetylhydrolase (PLA2G7) | ||||
| Synonyms |
gVIIA-PLA2; PAFAH; PAF acetylhydrolase; PAF 2-acylhydrolase; Lipoprotein-associated phospholipase A2; LDL-associated phospholipase A2; LDL-PLA(2); Group-VIIA phospholipase A2; 2-acetyl-1-alkylglycerophosphocholine esterase; 1-alkyl-2-acetylglycerophosphocholine esterase
Click to Show/Hide
|
||||
| Target Type | Clinical trial Target | ||||
| Gene Name | PLA2G7 | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
OXYQUINOLINE
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
8-HYDROXYQUINOLINE; quinolin-8-ol; 8-quinolinol; 148-24-3; Oxyquinoline; Oxine; Quinophenol; 8-Quinol; 8-Oxyquinoline; Phenopyridine; Oxychinolin; Bioquin; Oxybenzopyridine; Oxin; Hydroxybenzopyridine; 1-Azanaphthalene-8-ol; Tumex; 8-Chinolinol; 8-Hydroxychinolin; 8-OQ; 8-Hydroxy-chinolin; Fennosan H 30; Fennosan; o-Oxychinolin; 8-Oxychinolin; Usaf ek-794; Fennosan HF-15; NCI-C55298; NSC 2039; Oxyquinoline [USAN]; Caswell No. 719; Oxoquinoline; 8-Chinolinol [Czech]; o-Oxychinolin [German]; Quinoline, 8-hydroxy-; NSC 615011; UNII-5UTX5635HP
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-(6-Methyl-pyridin-3-ylmethyl)-2-(4-phenyl-butylsulfanyl)-1H-pyrimidin-4-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL129620; SCHEMBL7009527; BDBM50085618; 2-(4-Phenylbutylthio)-5-(6-methyl-3-pyridinylmethyl)-1,4-dihydropyrimidine-4-one; 5-[(6-methylpyridin-3-yl)methyl]-2-(4-phenylbutylsulfanyl)-1H-pyrimidin-6-one
Click to Show/Hide
|
||||
| Activity |
IC50 = 55000 nM
|
[2] | |||
| Compound Name |
8-(Methanesulfonamido)-4-oxo-N-[(1R)-1-phenylethyl]-1H-quinoline-2-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2335752; BDBM50429072
Click to Show/Hide
|
||||
| Activity |
IC50 = 86000 nM
|
[3] | |||
| Compound Name |
Xanthurenic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
4,8-Dihydroxyquinoline-2-carboxylic acid; Xanthuric acid; 8-Hydroxykynurenic acid; Xanthurenate; 4,8-Dihydroxyquinaldic acid; 4,8-Dihydroxyquinaldinic acid; 2-Quinolinecarboxylic acid, 4,8-dihydroxy-; 8-hydroxy-4-oxo-1H-quinoline-2-carboxylic acid; UNII-58LAB1BG8J; NSC 401570; QUINALDIC ACID, 4,8-DIHYDROXY-; 4,8-Dihydroxy-2-quinolinecarboxylic acid; NSC401570; 58LAB1BG8J; CHEMBL312535; CCRIS 4429; 4,8-Dihydroxyquinoline-2-carboxylate; 4,8-Dihydroxyquinoline-2-carboxylic acid, 96%; EINECS 200-410-1; BRN 0185954; Oxoxanthurenate; Xanthurate; 8-Hydroxykynurenate; 4-oxoxanthurenic acid; Spectrum_000253; 4,8-Dihydroxyquinaldate; Xanthurenic acid, 96%; Spectrum2_000158; Spectrum3_000143; Spectrum4_000117; Spectrum5_001562; 4,8-dihydroxy-Quinaldate; 4,8-Dihydroxyquinaldinate; Quinaldic acid,8-dihydroxy-; Oprea1_107134; BSPBio_001846; KBioGR_000474; KBioSS_000733; 4,8-dihydroxy-Quinaldic acid; BIDD:GT0640; DivK1c_000262; SCHEMBL379760; SPECTRUM1500754; SPBio_000296; CTK1H0426; HMS500N04; KBio1_000262; KBio2_000733; KBio2_003301; KBio2_005869; KBio3_001046; DTXSID90207728; NINDS_000262; HMS1921G08; HMS3885N22; WLN: T66 BNJ CVQ EQ JQ; ZINC8738372; 4,8-dihydroxyquinoline-2-carboxylic; 5527AH; ANW-43693; BDBM50113313; CCG-38363; KM0268; MFCD00006754; s4774; SBB003498; 4,8-Dihydroxy-2-quinolinecarboxylate; AKOS003237896; AKOS015894330; 4,8-dihydroxyquinolinium-2-carboxylate; ACN-049214; CS-W015382; HY-W014666; MCULE-1038310399; NSC-401570; SDCCGMLS-0066616.P001; 2-Quinolinecarboxylic acid,8-dihydroxy-; IDI1_000262; NCGC00094846-01; NCGC00094846-02; NCGC00094846-03; NCGC00094846-04; NCGC00094846-05; AS-56782; BP-10912; 2-Quinolinecarboxylicacid, 4,8-dihydroxy-; DB-053303; AM20061355; B7593; FT-0631263; ST45025626; Quinoline-2-carboxylic acid, 4,8-dihydroxy-; C02470; 4,8-Dihydroxy-quinoline-2-carboxylic acid anion; 059D007; A832107; SR-05000002445; 2-Quinolinecarboxylic acid, 4,8-dihydroxy- (9CI); CU-01000012491-3; Q5961262; SR-05000002445-1; BRD-K07327532-001-03-6; B5FF212D-76CB-4875-8A36-C67D8E69489C
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Zinquin ethyl ester
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
UNII-A806Y8IDMB; A806Y8IDMB; CHEMBL2335743; Ethyl 2-[2-methyl-8-[(4-methylphenyl)sulfonylamino]quinolin-6-yl]oxyacetate; Zinquin ethyl ester [MI]; Zinquin-E; SCHEMBL18132175; CTK8E8106; DTXSID60171164; ZINC2569542; BDBM50429090; MFCD00797629; AKOS027250764; AB0072339; FT-0675912; Zinquin ethyl ester, >=95% (HPLC), solid; J-008824; Q27273743; ethyl-[2-methyl-8-p-toluenesulfonamido-6-quinolyloxy]acetate
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
N-(6-Methoxy-8-quinolyl)-4-toluenesulfonamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
N-(6-methoxyquinolin-8-yl)-4-methylbenzenesulfonamide; N-(6-Methoxy-8-quinolyl)-p-toluenesulfonamide; UNII-7SWW052N6R; MLS000062611; 7SWW052N6R; N-(6-methoxy-8-quinolinyl)-4-methylbenzenesulfonamide; SMR000071147; TSQ-6N; 6-TSQ; NSC120213; 6-Methoxy-8-(4-toluenesulfonamide)quinoline; Oprea1_518427; Oprea1_781062; MLS001384814; cid_130606; SCHEMBL1505430; CHEMBL1445650; BDBM31074; DTXSID00148996; CX815; HMS2377L20; ZINC338359; 6-Methoxy-8-(tosylamino)quinoline; DNDI1417411; STK076443; AKOS000541587; MCULE-1951223603; NSC-120213; NCGC00056772-02; NCGC00056772-03; TG2-13-4; DB-081145; FT-0629257; ST50224806; MLS-0042289.0001; (R)-(+)-2-(4-Hydroxy Phenoxy)propionic acid; SR-01000397331; CU-01000060941-3; J-002312; Q7671630; SR-01000397331-1; N-(6-methoxy-8-quinolyl)-4-methyl-benzenesulfonamide; (6-methoxy(8-quinolyl))[(4-methylphenyl)sulfonyl]amine; (N-6-Methoxy-8-quinolinyl)-4-methylbenzene sulfonamide; F0347-2614; N-(6-methoxyquinolin-8-yl)-4-methyl-benzenesulfonamide; Benzenesulfonamide, N-(6-methoxy-8-quinolinyl)-4-methyl-
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
N-Cyclotetradecyl-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2335750; BDBM50429071
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
8-(Methanesulfonamido)-4-oxo-N-phenyl-1H-quinoline-2-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2335742; BDBM50429070
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
8-Hydroxy-4-oxo-N-phenyl-1H-quinoline-2-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1945882; BDBM50363379
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
8-Hydroxyquinoline-2-carboxanilide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1945883; BDBM50363380; CCG-196753; 8-hydroxy-N-phenyl-quinoline-2-carboxamide
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2'-Chloro-6-Methyl[1,1'-Biphenyl]-3-Amine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3819345; BDBM50182425; AKOS012639181; Q27456414; 6HX
Click to Show/Hide
|
||||
| Activity |
IC50 = 100000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 7 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
BENZENESULFONAMIDE
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
1998/10/2; Benzenesulphonamide; Benzosulfonamide; Benzolsulfonamide; phenyl sulfonamide; phenylsulfonamide; C6H7NO2S; M and B 7973; NSC 5341; EINECS 202-637-1; BRN 1100566; CHEMBL27601; AI3-04492; KHBQMWCZKVMBLN-UHFFFAOYSA-N; MFCD00007930; Benzenesulfonamide, 98+%; benzolsulfonamid; benzensulfonamide; phenylsulphonamide; 4jsa; 4jsz; 2wej; benzene sulphonamide; 1-benzenesulfonamide; Benzenesulfonyl amine; WLN: ZSWR; AC1Q6VDE; AC1L1OLV; benzenesulfonic acid amide; SCHEMBL729; EC 202
Click to Show/Hide
|
||||
| Activity |
IC50 > 1000000 nM
|
[4] | |||
| Compound Name |
8-Hydroxy-2-(piperidine-1-carbonyl)-1H-quinolin-4-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1946070; BDBM50363396
Click to Show/Hide
|
||||
| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
(2,5-Dihydro-1h-Pyrrol-1-Yl)(3-Fluorophenyl)methanone
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3818090; BDBM50182424; Q27456402; 6HO
Click to Show/Hide
|
||||
| Activity |
IC50 = 500000 nM
|
[4] | |||
| Compound Name |
N-(3,4-Difluorophenyl)methanesulfonamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4076637; N-[3,4-bis(fluoranyl)phenyl]methanesulfonamide; ZINC29686; BDBM50246902; STK083925; AKOS003253760; MCULE-1163881677; ST042732; (3,4-difluorophenyl)(methylsulfonyl)amine
Click to Show/Hide
|
||||
| Activity |
IC50 = 1000000 nM
|
[5] | |||
| Compound Name |
1-Methyl-3-(2-phenoxyethyl)imidazolidine-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1369790; MLS000035965; HMS1785L22; HMS2326L21; ZINC3297137; BDBM50197675; AKOS033626570; MCULE-4628014012; SMR000062612; SR-01000041169; SR-01000041169-1; Z18500398
Click to Show/Hide
|
||||
| Activity |
IC50 = 1000000 nM
|
[6] | |||
| Compound Name |
5,5-Dimethylhydantoin
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
5,5-dimethylimidazolidine-2,4-dione; 2,4-Imidazolidinedione, 5,5-dimethyl-; Dimethylhydantoin; DM Hydantoin; Dantoin DMH; 5,5-Dimethyl-2,4-imidazolidinedione; Dantoin 736; Hydantoin, 5,5-dimethyl-; 5,5-Dimethyl hydantoin; 5,5-Dimethylhydantoin (DMH); NSC 8652; UNII-34032MQ9RO; MFCD00005266; 5,5-Dimethylhydantoin, 97%; CHEMBL3181806; 34032MQ9RO; 4,4-dimethyl-2,5-dioxoimidazolidine; DSSTox_CID_1754; DSSTox_RID_76306; DSSTox_GSID_21754; HSDB 5216; EINECS 201-051-3; BRN 0002827; AI3-61127; 5,5-dimethyl-hydantoin; ACMC-209pb7; EC 201-051-3; SCHEMBL22069; 5-24-05-00348 (Beilstein Handbook Reference); KSC493Q2P; DTXSID5021754; CTK3J3827; NSC8652; WLN: T5MVMV EHJ E1 E1; ZINC391024; KS-00000C8C; NSC-8652; STR04524; Tox21_202049; Tox21_300361; 5,5-Dimethylimidazolidin-2,4-dione; ANW-37073; BBL010734; BDBM50182427; STK532811; 5,5-Dimethyl-imidazolidin-2,4-dion; 5,5-Dimethyl-imidazolidin-2,4-dione; AKOS000120928; 5,5-dimethyl-imidazolidine-2,4-dione; MCULE-9870409973; NE10391; N,N,N,N-Tetrabenzyl-p-phenylenediamine; NCGC00248006-01; NCGC00248006-02; NCGC00254403-01; NCGC00259598-01; 5,5-Dimethylhydantoin; LC-tDDA; CE10; AK-44101; SC-26750; 5,5-dimethyl-1,3-diazolidine-2,4-dione; D0739; FT-0619787; ST50409571; Q-200523; Q27256302; F1908-0098
Click to Show/Hide
|
||||
| Activity |
IC50 > 1000000 nM
|
[4] | |||
| Compound Name |
1,3-Dimethyl-6-(2-Methylpropoxy)pyrimidine-2,4(1h,3h)-Dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3819543; BDBM50182426; Q27456403; 6HP
Click to Show/Hide
|
||||
| Activity |
IC50 = 1000000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2). Bioorg Med Chem Lett. 2012 Jan 15;22(2):868-71. | ||||
| REF 2 | 2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett. 2000 Feb 21;10(4):395-8. | ||||
| REF 3 | Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA1 . Bioorg Med Chem Lett. 2013 Mar 1;23(5):1553-6. | ||||
| REF 4 | Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening. J Med Chem. 2016 Jun 9;59(11):5356-67. | ||||
| REF 5 | Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2. J Med Chem. 2017 Dec 28;60(24):10231-10244. | ||||
| REF 6 | Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA 2). J Med Chem. 2016 Dec 8;59(23):10738-10749. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.