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Literature summary for 5.3.99.3 extracted from

  • Muthukaman, N.; Tambe, M.; Deshmukh, S.; Pisal, D.; Tondlekar, S.; Shaikh, M.; Sarode, N.; Kattige, V.G.; Pisat, M.; Sawant, P.; Honnegowda, S.; Karande, V.; Kulkarni, A.; Behera, D.; Jadhav, S.B.; Sangana, R.R.; Gudi, G.S.; Khairatkar-Joshi, N.; Gharat, L.A.
    Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors Part-1 (2017), Bioorg. Med. Chem. Lett., 27, 5131-5138 .
    View publication on PubMed
Search for more literature for 5.3.99.3

Inhibitors

Inhibitors Comment Organism Structure
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide PF-4693627 Homo sapiens
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile MF-63 Homo sapiens
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
MF-63
-
 Homo sapiens
N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
-
 Homo sapiens
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
 Homo sapiens
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
 Homo sapiens
PF-4693627
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Prostaglandin H2 Homo sapiens
-
 Prostaglandin E2
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O14684
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Prostaglandin H2
-
 Homo sapiens Prostaglandin E2
-
 ?

Synonyms

Synonyms Comment Organism
microsomal prostaglandin E synthase-1
-
 Homo sapiens
mPGES-1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000009
-
 pH and temperature not specified in the publication Homo sapiens 2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
0.000001
-
 pH and temperature not specified in the publication Homo sapiens 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
0.0000022
-
 pH and temperature not specified in the publication Homo sapiens N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000023
-
 pH and temperature not specified in the publication Homo sapiens N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000028
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000003
-
 pH and temperature not specified in the publication Homo sapiens 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
0.0000035
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000037
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000037
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000039
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000004
-
 pH and temperature not specified in the publication Homo sapiens N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
0.0000041
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000042
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000046
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000047
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000005
-
 pH and temperature not specified in the publication Homo sapiens N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
0.0000058
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000062
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000063
-
 pH and temperature not specified in the publication Homo sapiens N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000065
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000067
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.0000077
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000008
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
0.0000094
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.00001
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000011
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000013
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000013
-
 pH and temperature not specified in the publication Homo sapiens N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000017
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.00002
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000021
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000022
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000023
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000025
-
 pH and temperature not specified in the publication Homo sapiens N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000026
-
 pH and temperature not specified in the publication Homo sapiens N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000047
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000058
-
 pH and temperature not specified in the publication Homo sapiens 2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000082
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
0.000157
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide