Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T14834 | Target Info | |||
| Target Name | Cytosolic phospholipase A2 (GIVA cPLA2) | ||||
| Synonyms |
Phospholipase A2 group IVA; PLA2G4; CPLA2
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| Target Type | Clinical trial Target | ||||
| Gene Name | PLA2G4A | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 17 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Zafirlukast
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Approved | Compound Info | ||
| Synonyms |
Accolate; Accoleit; Aeronix; Olmoran; Respix; Zafirst; AstraZeneca brand of zafirlukast; Menarini brand of zafirlukast; Novartis brand of zafirlukast; Zeneca brand of zafirkulast; Accolate (TN); Accoleit (TN); Vanticon (TN); Zafirlukast [USAN:BAN:INN]; Accolate, Accoleit, Vanticon, Zafirlukast; Zafirlukast (JAN/USAN/INN); Cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate; Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate; Cyclopentyl 3-[2-methoxy-4-(2-methylphenylsulfonylcarbamoyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate; Cyclopentyl [3-(2-methoxy-4-{[(2-methylphenyl)sulfonyl]carbamoyl}benzyl)-1-methyl-1H-indol-5-yl]carbamate; Cyclopentyl (1-methyl-3-{[2-(methyloxy)-4-({[(2-methylphenyl)sulfonyl]amino}carbonyl)phenyl]methyl}-1H-indol-5-yl)carbamate; Carbamic acid, (3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, cyclopentyl ester; 4-(5-cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-N-O-tolylsulfonylbenzamide
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| Activity |
IC50 = 85000 nM
|
[1] | |||
| Compound Name |
4-[2-[5-Chloro-1-(diphenylmethyl)-2-phenyl-1H-indol-3-yl]ethoxy]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL378803; BDBM50180092
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-(2-(2-(1,3-Diphenylpropan-2-yl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl)ethoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL426678; BDBM50184566
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-(2-(2-(2,2-Diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl)ethoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL382896; BDBM50184565
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-(4-(2-(2,2-Diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl)butoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL210197; BDBM50184559
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-(4-(2-(2,2-Diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl)but-2-enyloxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL208570; BDBM50184553
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-(2-(3-Benzhydryl-2,4,6-trioxo-5-phenyl-1,3,5-triazinan-1-yl)ethoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL207279; BDBM50184562
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-(2-(2-Benzhydryl-3,5-dioxo-1,2,4-oxadiazolidin-4-yl)ethoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL207998; BDBM50184558
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
6-[2-[5-Chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]-ethoxy]nicotinic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL381944; BDBM50180089
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| Activity |
IC50 = 85000 nM
|
[2] | |||
| Compound Name |
4-[2-[2-[2-(Benzylsulfonylamino)ethyl]-5-chloro-1-propan-2-ylindol-3-yl]ethoxy]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL374423; BDBM50205544; 4-[2-(2-{2-[benzylsulfonyl)amino]ethyl}-5-chloro-1-isopropyl-1H-indole-3-yl)ethoxy]benzoic acid
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| Activity |
IC50 = 90000 nM
|
[4] | |||
| Compound Name |
3-(3-(1-Benzhydryl-6-chloro-1H-indol-3-yl)-2-hydroxypropyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL203311; BDBM50180094
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| Activity |
IC50 = 90000 nM
|
[2] | |||
| Compound Name |
4-[2-[[2-[5-Chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]ethyl]sulfonyl]ethyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL199979; BDBM50180095
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| Activity |
IC50 = 93000 nM
|
[2] | |||
| Compound Name |
3-[1-Phenyl-3-(2-phenylethyl)indol-5-yl]propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3326958; SCHEMBL3116937; BDBM50056720
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
3-((1-Benzhydryl-6-chloro-1H-indol-3-yl)methyl)-2-methoxybenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL201524; BDBM50180090
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| Activity |
IC50 = 120000 nM
|
[2] | |||
| Compound Name |
3-[2-[5-Chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]-ethoxy]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL201535; BDBM50180060
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| Activity |
IC50 = 120000 nM
|
[2] | |||
| Compound Name |
3-Methoxy-4-(1-benzhydryl-6-chloro-1H-indole-3-ylmethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL139858; SCHEMBL3681683; BDBM50136730; 4-[(1-benzhydryl-6-chloroindol-3-yl)methyl]-3-methoxybenzoic acid; 4-((1-benzhydryl-6-chloro-1H-indol-3-yl)methyl)-3-methoxybenzoic acid; 4-(1-Benzhydryl-6-chloro-1H-indol-3-ylmethyl)-3-methoxy-benzoic acid
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| Activity |
IC50 = 160000 nM
|
[2] | |||
| Compound Name |
[5-Chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL371299; CTK3C5064; DTXSID90470334; BDBM50180078; 1H-Indole-3-acetic acid, 5-chloro-1-(diphenylmethyl)-2-methyl-
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| Activity |
IC50 = 165000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-(2-Hydroxy-3-{4-[(5-phenylpentyl)sulfanyl]phenoxy}propoxy)benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL199534; CTK3C5055; DTXSID50658772; BDBM50180061; 4-(2-hydroxy-3-(4-(5-phenylpentylthio)phenoxy)propoxy)benzoic acid; Benzoic acid, 4-[2-hydroxy-3-[4-[(5-phenylpentyl)thio]phenoxy]propoxy]-
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| Activity |
IC50 = 340000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4501-4. | ||||
| REF 2 | Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization. J Med Chem. 2006 Jan 12;49(1):135-58. | ||||
| REF 3 | 1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A2alpha inhibitors. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2978-81. | ||||
| REF 4 | Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha. J Med Chem. 2007 Mar 22;50(6):1380-400. | ||||
| REF 5 | Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2alpha inhibitors. J Med Chem. 2014 Sep 11;57(17):7244-62. | ||||
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