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Literature summary for 2.5.1.58 extracted from

  • Bendale, P.; Olepu, S.; Suryadevara, P.K.; Bulbule, V.; Rivas, K.; Nallan, L.; Smart, B.; Yokoyama, K.; Ankala, S.; Pendyala, P.R.; Floyd, D.; Lombardo, L.J.; Williams, D.K.; Buckner, F.S.; Chakrabarti, D.; Verlinde, C.L.; Van Voorhis, W.C.; Gelb, M.H.
    Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials (2007), J. Med. Chem., 50, 4585-4605.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1,5-dimethyl-1H-imidazole-4-sulfonic acid (5-bromo-2-fluorobenzyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide 98% inhibition at 50 nM Plasmodium falciparum
1,5-dimethyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-ethanesulfonyl-benzyl)-amide 97% inhibition at 50 nM Plasmodium falciparum
1,5-dimethyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide 92% inhibition at 50 nM Plasmodium falciparum
1-(2-chlorophenyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(methylsulfonyl)benzyl]methanesulfonamide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid (2-bromo-allyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-amide 97% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid (2-bromo-allyl)-[6-cyano-1-(3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide 94% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid (4-benzenesulfonylbenzyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid (4-methanesulfonylbenzyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-amide 98% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid benzyl-[6-cyano-1-(3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide 93% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid ethyl-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]amide 86% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-pyrrol-1-yl-ethyl)-amide 90% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-yl-methyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methoxy-propyl)-amide
-
Rattus norvegicus
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4,4-dioxo-3,4-dihydro-2H-4lambda6-benzo[1,4]oxathin-7-ylmethyl)-amide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-ethanesulfonyl-benzyl)-amide complete inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-fluoro-benzyl)-amide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide complete inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(5-trifluoromethyl-furan-2-ylmethyl)-amide 97% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-fluoro-phenyl)-ethyl]-amide complete inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-oxo-pyrrolidin-1-yl)-ethyl]-amide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(4-fluoro-phenyl)-ethyl]-amide complete inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[4-(1,3-dioxo-1,3-dihydro-isoindol-2-yloxy)-butyl]-amide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-1H-pyrazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-fluoro-benzyl)-amide 94% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-(2-methylbenzyl)-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 46% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 80% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-methylprop-2-en-1-yl)-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-prop-2-en-1-yl-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-prop-2-yn-1-yl-1H-imidazole-4-sulfonamide 95% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide 79% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
-
Rattus norvegicus
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(methylsulfonyl)ethyl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[[5-(trifluoromethyl)furan-2-yl]methyl]-1H-imidazole-4-sulfonamide 88% inhibition at 50 nM Plasmodium falciparum
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 32% inhibition at 50 nM Plasmodium falciparum
1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
-
Rattus norvegicus
1-methylethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 97% inhibition at 50 nM Plasmodium falciparum
2,2,2-trifluoroethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 91% inhibition at 50 nM Plasmodium falciparum
2-methylpropyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 98% inhibition at 50 nM Plasmodium falciparum
2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)amino]-2-oxoethyl acetate 33% inhibition at 50 nM Plasmodium falciparum
3,4-dihydro-2H-benzo[b][1,4]dioxepine-7-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide 97% inhibition at 50 nM Plasmodium falciparum
3-methyl-3H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide complete inhibition at 50 nM Plasmodium falciparum
3-methyl-thiophene-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide 97% inhibition at 50 nM Plasmodium falciparum
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid 80% inhibition at 50 nM Plasmodium falciparum
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid benzylamide 59% inhibition at 50 nM Plasmodium falciparum
3-[(tert-butylcarbamoyl-methyl)-(1-methyl-1H-imidazol-4-sulfonyl)-amino]-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-6-carboxylic acid tert-butylamide 25% inhibition at 50 nM Plasmodium falciparum
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-N-(1-methylpropyl)-1,2,3,4-tetrahydroquinoline-6-carboxamide 35% inhibition at 50 nM Plasmodium falciparum
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N,N-diethyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide 69% inhibition at 50 nM Plasmodium falciparum
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-(1-methylethyl)-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide 46% inhibition at 50 nM Plasmodium falciparum
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-cyclohexyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide 66% inhibition at 50 nM Plasmodium falciparum
3-[[2-(tert-butylamino)-2-oxoethyl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]-N-methyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinoline-6-carboxamide 69% inhibition at 50 nM Plasmodium falciparum
4-([(2-carboxy-furan-5-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 89% inhibition at 50 nM Plasmodium falciparum
4-([(benzo[1,2,5]oxadiazole-4-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 99% inhibition at 50 nM Plasmodium falciparum
4-([(benzo[1,2,5]thiadiazole-4-sulfonyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 98% inhibition at 50 nM Plasmodium falciparum
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-cyclopropanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 37% inhibition at 50 nM Plasmodium falciparum
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-ethanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 44% inhibition at 50 nM Plasmodium falciparum
4-([[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-methanesulfonylmethanesulfonyl-amino]-methyl)-piperidine-1-carboxylic acid methyl ester 15% inhibition at 50 nM Plasmodium falciparum
4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]benzoic acid 66% inhibition at 50 nM Plasmodium falciparum
4-[[(6-cyano-1-pyridin-3-ylmethyl-1,2,3,4-tetrahydro-quinolin-3-yl)-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester 35% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1,5-dimethyl-1H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester complete inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1,5-dimethyl-1H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester 98% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-oxo-2H-chromene-6-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester 68% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3,4-dihydro-2H-benzo[b][1,4]dioxepine-7-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester 99% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methyl-3H-imidazole-4-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester 99% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid ethylamide 98% inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester complete inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
-
Rattus norvegicus
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester complete inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
Rattus norvegicus
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N,N-dimethylpiperidine-1-carboxamide complete inhibition at 50 nM Plasmodium falciparum
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N-(1-methylethyl)piperidine-1-carboxamide complete inhibition at 50 nM Plasmodium falciparum
6-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)hexanamide 98% inhibition at 50 nM Plasmodium falciparum
6-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]hexanamide 81% inhibition at 50 nM Plasmodium falciparum
6-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-pyridine-2-carboxylic acid methyl ester 96% inhibition at 50 nM Plasmodium falciparum
6-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]pyridine-2-carboxylic acid 97% inhibition at 50 nM Plasmodium falciparum
benzyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 98% inhibition at 50 nM Plasmodium falciparum
ethyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 98% inhibition at 50 nM Plasmodium falciparum
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate complete inhibition at 50 nM Plasmodium falciparum
ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
-
Rattus norvegicus
methyl 2-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]pyridine-4-carboxylate complete inhibition at 50 nM Plasmodium falciparum
methyl 4-[([(2-chlorophenyl)sulfonyl][6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]amino)methyl]piperidine-1-carboxylate 97% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1,2-dimethyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate complete inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 96% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]benzoate 62% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 97% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-pyrazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate complete inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(3-fluorophenyl)sulfonyl]amino)methyl]piperidine-1-carboxylate 93% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(3-methylthiophen-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 95% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(4-methoxyphenyl)sulfonyl]amino)methyl]piperidine-1-carboxylate 98% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(4-methylthiophen-2-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 99% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][[3-(methoxycarbonyl)thiophen-2-yl]sulfonyl]amino)methyl]piperidine-1-carboxylate 92% inhibition at 50 nM Plasmodium falciparum
methyl 4-[([[4-(acetylamino)phenyl]sulfonyl][6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]amino)methyl]piperidine-1-carboxylate 65% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 98% inhibition at 50 nM; complete inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](dimethylsulfamoyl)amino]methyl]piperidine-1-carboxylate 58% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](methylsulfonyl)amino]methyl]piperidine-1-carboxylate 66% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](naphthalen-1-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 88% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](phenylsulfonyl)amino]methyl]piperidine-1-carboxylate 98% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](propylsulfonyl)amino]methyl]piperidine-1-carboxylate 55% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-3-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 99% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](quinolin-8-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 95% inhibition at 50 nM Plasmodium falciparum
methyl 4-[[[6-cyano-1-[1-(1H-imidazol-5-yl)ethyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 69% inhibition at 50 nM Rattus norvegicus
methyl [2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]ethyl]carbamate 90% inhibition at 50 nM Plasmodium falciparum
methyl [3-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)propyl]carbamate complete inhibition at 50 nM Plasmodium falciparum
methyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]carbamate 96% inhibition at 50 nM Plasmodium falciparum
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]carbamate 99% inhibition at 50 nM Plasmodium falciparum
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]ethylcarbamate 89% inhibition at 50 nM Plasmodium falciparum
methyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]methylcarbamate 90% inhibition at 50 nM Plasmodium falciparum
methyl [6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)carbamate 26% inhibition at 50 nM Plasmodium falciparum
additional information not inhibited by 4-[[[6-cyano-1-(3-methyl-3H-imidazole-4-sulfonyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester Plasmodium falciparum
N,1-dimethyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 88% inhibition at 50 nM Plasmodium falciparum
N-(2,1,3-benzothiadiazol-4-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-(2,1,3-benzothiadiazol-4-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 85% inhibition at 50 nM Plasmodium falciparum
N-(2,1,3-benzoxadiazol-5-ylmethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-(2-aminoethyl)-4-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)butanamide
-
Plasmodium falciparum
N-(2-aminoethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 72% inhibition at 50 nM Plasmodium falciparum
N-(2-aminoethyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 65% inhibition at 50 nM Plasmodium falciparum
N-(2-chloroprop-2-en-1-yl)-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-(2-fluorobenzyl)-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-(3-aminopropyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 60% inhibition at 50 nM Plasmodium falciparum
N-(4-bromobenzyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 66% inhibition at 50 nM Plasmodium falciparum
N-(4-bromophenyl)-4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide 38% inhibition at 50 nM Plasmodium falciparum
N-(4-cyanobenzyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-([1-[(4-chlorophenyl)carbonyl]piperidin-4-yl]methyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide 26% inhibition at 50 nM Plasmodium falciparum
N-benzyl-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-butyl-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 32% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-2-[(1-methyl-1H-imidazole-4-sulfonyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-acetamide 97% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-4-[[[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide 22% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxamide 98% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(methylsulfonyl)glycinamide 2% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(phenylsulfonyl)glycinamide 8% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide 11% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(thiophen-2-ylsulfonyl)glycinamide 10% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 80% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
-
Rattus norvegicus
N-tert-butyl-N2-[6-cyano-1-(1H-imidazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 15% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-(2,4-dimethyl-1,3-thiazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 3% inhibition at 5 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-(4-fluorophenyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 71% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-(5-methylisoxazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 3% inhibition at 50 nM Plasmodium falciparum
N-tert-butyl-N2-[6-cyano-1-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 60% inhibition at 50 nM Plasmodium falciparum
N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide 94% inhibition at 50 nM Plasmodium falciparum
N-[(1-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 69% inhibition at 50 nM Plasmodium falciparum
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide 95% inhibition at 50 nM Plasmodium falciparum
N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[(2E)-but-2-en-1-yl]-1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 55% inhibition at 50 nM Plasmodium falciparum
N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 90% inhibition at 50 nM Plasmodium falciparum
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 53% inhibition at 50 nM Plasmodium falciparum
N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide 19% inhibition at 50 nM Plasmodium falciparum
N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[2-chloro-4-(methylsulfonyl)benzyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](2-fluorobenzyl)sulfamoyl]phenyl]acetamide 25% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(1,2,3-thiadiazol-5-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide 66% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(1H-imidazol-5-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide 88% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-2-dimethylamino-N-(2-fluoro-benzyl)-acetamide 16% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(2-fluoro-benzyl)-3-methylsulfanylpropionamide 52% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(2-fluoro-benzyl)-4-methoxy-benzenesulfonamide 66% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-N-(4-methanesulfonyl-benzyl)-benzenesulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-([1-[(1-methyl-1H-imidazol-4-yl)sulfonyl]piperidin-4-yl]methyl)pyridine-2-sulfonamide 92% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[(1-propanoylpiperidin-4-yl)methyl]pyridine-2-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylacryloyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylpropanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopentylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopropylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(ethylsulfonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(furan-3-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 92% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(methylsulfonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 94% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 94% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(thiophen-3-ylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-methylbenzyl)-1H-imidazole-4-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-phenylethyl)-1H-imidazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-piperidin-1-ylethyl)-1H-imidazole-4-sulfonamide 93% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(2-thiophen-3-ylethyl)-1H-imidazole-4-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(piperidin-4-ylmethyl)-1H-imidazole-4-sulfonamide 65% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(pyridin-2-ylmethyl)-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(pyridin-3-ylmethyl)-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(quinolin-7-ylmethyl)-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-(thiophen-3-ylmethyl)-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[(5-phenyl-1,3-oxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide 92% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-(1H-pyrrol-1-yl)ethyl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-(trifluoromethyl)benzyl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[2-[2-(trifluoromethyl)phenyl]ethyl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-1,2,4-triazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide 93% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrrol-1-yl)benzyl]-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-pyrazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[[5-(trifluoromethyl)furan-2-yl]methyl]-1H-imidazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-3-fluoro-N-[4-(methylsulfonyl)benzyl]benzenesulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-4-methoxy-N-[4-(methylsulfonyl)benzyl]benzenesulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-ethoxybenzyl)-1-methyl-1H-imidazole-4-sulfonamide 11% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-carboxamide 92% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide 96% inhibition at 50 nM; complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-2,1,3-benzothiadiazole-4-sulfonamide 74% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-2-methoxyacetamide 56% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-3-(methylsulfanyl)propanamide 52% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-N',N'-dimethylsulfamide 62% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)acetamide 43% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)benzenesulfonamide 86% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)cyclopropanecarboxamide 33% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)ethanesulfonamide 61% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)methanesulfonamide 51% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)propane-1-sulfonamide 41% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)pyridine-2-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-methylbenzyl)pyridine-2-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(3-methoxypropyl)pyridine-2-sulfonamide 93% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(5-methoxypentyl)pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylsulfonyl)glycine 81% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-3-ylmethyl)pyridine-2-sulfonamide 15% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(quinolin-8-ylmethyl)pyridine-2-sulfonamide 88% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)sulfonyl]glycine 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(2-phenyl-2H-1,2,3-triazol-4-yl)methyl]pyridine-2-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(3,5-dimethylisoxazol-4-yl)methyl]-1-methyl-1H-imidazole-4-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide 98% inhibition at 50 nM; complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)methyl]pyridine-2-sulfonamide 94% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-imidazol-1-yl)ethyl]pyridine-2-sulfonamide 95% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-indol-3-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
-
Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,3-dihydro-1,4-benzodioxin-5-yloxy)ethyl]pyridine-2-sulfonamide 88% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,3-dihydro-1H-indol-1-yl)ethyl]pyridine-2-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2,5-dihydrothiophen-3-yl)ethyl]-1-methyl-1H-imidazole-4-sulfonamide complete inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(2-fluorophenyl)ethyl]pyridine-2-sulfonamide 98% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(4-fluorophenyl)ethyl]pyridine-2-sulfonamide 96% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(5,5-dimethyl-1,3-dioxan-2-yl)ethyl]pyridine-2-sulfonamide 95% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(dimethylamino)ethyl]-1-methyl-1H-imidazole-4-sulfonamide 64% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(trifluoromethyl)benzyl]pyridine-2-sulfonamide 91% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-1,2,4-triazol-1-yl)benzyl]pyridine-2-sulfonamide 53% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-pyrazol-1-yl)benzyl]pyridine-2-sulfonamide 90% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(1H-pyrrol-1-yl)benzyl]pyridine-2-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[3-(dimethylamino)propyl]-1-methyl-1H-imidazole-4-sulfonamide 34% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butyl]-1-methyl-1H-imidazole-4-sulfonamide 97% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butyl]pyridine-2-sulfonamide 92% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(3,4-dimethyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)butyl]pyridine-2-sulfonamide 90% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)oxy]butyl]-1-methyl-1H-imidazole-4-sulfonamide 99% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)oxy]butyl]pyridine-2-sulfonamide 84% inhibition at 50 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[[5-(trifluoromethyl)furan-2-yl]methyl]pyridine-2-sulfonamide 84% inhibition at 50 nM Plasmodium falciparum
N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-N-(3-methoxypropyl)-1-methyl-1H-imidazole-4-sulfonamide
-
Plasmodium falciparum
N2-[1-(2-aminoethyl)-6-cyano-1,2,3,4-tetrahydroquinolin-3-yl]-N-tert-butyl-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 11% inhibition at 50 nM Plasmodium falciparum
N2-[1-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]-6-cyano-1,2,3,4-tetrahydroquinolin-3-yl]-N-tert-butyl-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide 11% inhibition at 50 nM Plasmodium falciparum
N2-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N2-(pyridin-2-ylsulfonyl)glycinamide 82% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid (1-benzenesulfonyl-piperidin-4-ylmethyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-amide
-
Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methanesulfonyl-piperidin-4-ylmethyl)-amide 99% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(2-pyrazol-1-ylethyl)-amide 99% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-fluoro-benzyl)-amide 91% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(4-methanesulfonyl-benzyl)-amide 96% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-piperidin-4-ylmethylamide 18% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(2,2-dimethylpropionyl)-piperidin-4-ylmethyl]-amide 99% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(3,3,3-trifluoropropionyl)-piperidin-4-ylmethyl]-amide 98% inhibition at 50 nM Plasmodium falciparum
pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[2-(2-trifluoromethyl-phenyl)-ethyl]-amide 95% inhibition at 50 nM Plasmodium falciparum
tert-butyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 33% inhibition at 50 nM Plasmodium falciparum
tert-butyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate 69% inhibition at 50 nM Rattus norvegicus
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(phenylcarbonyl)glycinate
-
Plasmodium falciparum
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)carbonyl]glycinate
-
Plasmodium falciparum
tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)carbonyl]glycinate
-
Plasmodium falciparum
tert-butyl [2-([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)ethyl]carbamate 98% inhibition at 50 nM Plasmodium falciparum
tert-butyl [2-([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)ethyl]carbamate 99% inhibition at 50 nM Plasmodium falciparum
tert-butyl [2-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]ethyl]carbamate 91% inhibition at 50 nM Plasmodium falciparum
tert-butyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]carbamate 97% inhibition at 50 nM Plasmodium falciparum
tert-butyl [3-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]propyl]methylcarbamate 86% inhibition at 50 nM Plasmodium falciparum
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]carbamate 97% inhibition at 50 nM Plasmodium falciparum
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]ethylcarbamate 92% inhibition at 50 nM Plasmodium falciparum
tert-butyl [4-[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]butyl]methylcarbamate 98% inhibition at 50 nM Plasmodium falciparum
tetrahydroquinoline
-
Plasmodium falciparum
tetrahydroquinoline
-
Rattus norvegicus
[(1-methyl-1H-imidazole-4-sulfonyl)-[1-(3-methyl-3H-imidazol-4-ylmethyl)-6-phenyl-1,2,3,4-tetrahydro-quinolin-3-yl]-amino]-acetic acid methyl ester 99% inhibition at 50 nM Plasmodium falciparum
[2-(4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 88% inhibition at 50 nM Plasmodium falciparum
[3-[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-propyl]-methyl-carbamic acid methyl ester 95% inhibition at 50 nM Plasmodium falciparum
[[1-(3-benzyl-3H-imidazol-4-ylmethyl)-6-cyano-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methyl-1H-imidazole-4-sulfonyl)-amino]-acetic acid tert-butyl ester 45% inhibition at 5 nM Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
partially purified Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + biotin-YRASNRSCAIM
-
Rattus norvegicus diphosphate + biotin-YRASNRS-(S-farnesyl)CAIM
-
?
farnesyl diphosphate + biotin-YRASNRSCAIM
-
Plasmodium falciparum diphosphate + biotin-YRASNRS-(S-farnesyl)CAIM
-
?

Synonyms

Synonyms Comment Organism
PFT
-
Rattus norvegicus
PFT
-
Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000029
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.0000005
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
0.0000005
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.00000058
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum 4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
0.0000006
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.0000006
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(2-methylpropanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.00000065
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum 4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid ethylamide
0.00000075
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(cyclopropylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.0000008
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[(1-propanoylpiperidin-4-yl)methyl]pyridine-2-sulfonamide
0.0000009
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(1-methanesulfonyl-piperidin-4-ylmethyl)-amide
0.0000012
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(2,2-dimethylpropionyl)-piperidin-4-ylmethyl]-amide
0.0000014
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum 4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
0.0000017
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[2-(1H-pyrrol-1-yl)ethyl]pyridine-2-sulfonamide
0.000002
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-[1-(3,3,3-trifluoropropionyl)-piperidin-4-ylmethyl]-amide
0.0000024
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[(1-acetylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
0.0000026
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-pyrazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
0.0000027
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum methyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.000003
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(4-phenyl-1,3-oxazol-5-yl)methyl]pyridine-2-sulfonamide
0.000003
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
0.0000032
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus 4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid methyl ester
0.0000034
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus 1-methyl-N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-4-yl)methyl]-1H-imidazole-4-sulfonamide
0.0000038
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(pyridin-2-ylmethyl)pyridine-2-sulfonamide
0.0000048
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus 1-methylethyl 4-[([1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate
0.000005
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
0.000005
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(1H-1,2,4-triazol-1-yl)benzyl]-1H-imidazole-4-sulfonamide
0.0000055
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus ethyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.0000065
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[(1-butanoylpiperidin-4-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
0.000007
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus tert-butyl 4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]piperidine-1-carboxylate
0.000007
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.0000075
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus 1-methyl-1H-imidazole-4-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-yl-methyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(3-methoxy-propyl)-amide
0.0000078
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(3,3-dimethylbutanoyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.000008
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-tert-butyl-N2-[6-cyano-1-(1-methyl-1H-imidazol-5-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
0.00001
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[(6-chloro-2,1,3-benzothiadiazol-5-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
0.000016
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]-N-[[1-(phenylcarbonyl)piperidin-4-yl]methyl]pyridine-2-sulfonamide
0.000025
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus 4-[[[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-(pyridine-2-sulfonyl)-amino]-methyl]-piperidine-1-carboxylic acid isobutyl ester
0.000042
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-tert-butyl-N2-[6-cyano-1-(4-fluorophenyl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
0.00005
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(phenylcarbonyl)glycinate
0.00005
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(1-methyl-1H-imidazol-4-yl)carbonyl]glycinate
0.00005
-
IC50 above 0.00005 mM, at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum tert-butyl N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-[(5-methylisoxazol-3-yl)carbonyl]glycinate
0.000105
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[1-[(1-methyl-1H-imidazol-5-yl)methyl]-6-phenyl-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
0.00044
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[(3-bromonaphthalen-2-yl)methyl]-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]pyridine-2-sulfonamide
0.0008
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-tert-butyl-N2-[6-cyano-1-(1H-imidazol-4-yl)-1,2,3,4-tetrahydroquinolin-3-yl]-N2-[(1-methyl-1H-imidazol-2-yl)sulfonyl]glycinamide
0.0009
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, and 0.01% Triton X-100 Plasmodium falciparum N-([1-[(4-chlorophenyl)carbonyl]piperidin-4-yl]methyl)-N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl]pyridine-2-sulfonamide
0.001
-
at pH 7.5, in 50 mM HEPES, 30 mM MgCl2, 20 mM KCl, 5 mM dithiothreitol, 0.01% Triton X-100 Rattus norvegicus N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl]-N-(2-fluorobenzyl)-1-methyl-1H-imidazole-4-sulfonamide