2.1.1.45 additional information - additional information DHFR inhibition kinetics 742057 2.1.1.45 0.00000006 - D1694 - 485413 2.1.1.45 0.000000095 - methotrexate pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.000000597 - trimetrexate pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.000001 - 5-fluoro-2'-deoxyuridylic acid - 485414 2.1.1.45 0.000001 - D1694 pentaglutamate - 485413 2.1.1.45 0.0000015 - D1694 pentaglutamate - 485413 2.1.1.45 0.0000017 - 5-fluoro-2'-deoxyuridylic acid - 485413 2.1.1.45 0.000002 - 5-fluoro-2'-deoxyuridine 5'-monophosphate 22°C 694812 2.1.1.45 0.000002 - 5-fluoro-2'-deoxyuridine 5'-monophosphate inhibited both ThyA and ThyX 694812 2.1.1.45 0.000002 - 5-fluoro-2'-deoxyuridylic acid - 485413 2.1.1.45 0.0000028 - D1694 - 485413 2.1.1.45 0.000004 - 5-fluoro-2'-deoxyuridylic acid - 485358 2.1.1.45 0.000004 - Cibacron blue - 485384 2.1.1.45 0.000005 - 5-fluoro-2'-deoxyuridylic acid - 485384, 485393, 485411 2.1.1.45 0.0000059 - propylene diphosphonate wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C 720995 2.1.1.45 0.00000635 - pyrimethamine pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.00001 - 5-Formyl-2'-deoxyuridylic acid - 485375 2.1.1.45 0.00001 - 5-Mercapto-2'-deoxyuridylic acid - 485415 2.1.1.45 0.00001 - 5-trifluoromethyl-2'-deoxyuridylic acid - 485375 2.1.1.45 0.0000113 - propylene diphosphonate mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C 720995 2.1.1.45 0.000012 - 5-Formyl-2'-deoxyuridylic acid - 485365 2.1.1.45 0.000013 - 5-Formyl-2'-deoxyuridylic acid - 485365 2.1.1.45 0.000014 - 5-fluoro-2'-deoxyuridine 5'-monophosphate - 485378 2.1.1.45 0.0000176 - trimethoprim pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.000018 - (2R)-2-(5-[[(1-hydroxy-3-methyl-5,10a-dihydrobenzo[f]quinazolin-9-yl)methyl]amino]-1-oxo-1,3-dihydro-2H-isoindol-2-yl)butanedioic acid 22°C 694812 2.1.1.45 0.000018 - GW1843U89 - 694812 2.1.1.45 0.00002 - 5-fluoro-2'-deoxyuridylic acid L1210 parental enzyme 485427 2.1.1.45 0.000021 - 5-fluoro-2'-deoxyuridylic acid 50 nM 485404 2.1.1.45 0.0000235 - 5-fluoro-2'-deoxyuridylic acid - 485404 2.1.1.45 0.000026 - 5-fluoro-2'-deoxyuridylic acid 200 nM 485404 2.1.1.45 0.000029 - 5-Nitro-2'-deoxyuridine 5'-monophosphate - 485378 2.1.1.45 0.000038 - ZD9331 pH 7.2, 22°C 690892 2.1.1.45 0.000039 - 5-trifluoromethyl-2'-deoxyuridine 5'-monophosphate - 485378 2.1.1.45 0.00004 - 5-Mercapto-2'-deoxyuridylic acid - 485375 2.1.1.45 0.00005 - 5-fluoro-2'-deoxyuridylic acid - 485389 2.1.1.45 0.00009 - CB3717 - 485420 2.1.1.45 0.0000931 - raltitrexed pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.0001 - 10-Formyltetrahydrofolylheptaglutamate - 485398 2.1.1.45 0.0001 - 5-fluoro-2'-deoxyuridine 5'-monophosphate 22°C 694812 2.1.1.45 0.0001 - Procion blue variable substrate 2'-deoxyuridine 485393 2.1.1.45 0.00012 - tetrahydromethotrexate - 485373 2.1.1.45 0.00022 - Procion blue variable substrate 5,10-methylenetetrahydropteroylglutamate 485393 2.1.1.45 0.00029 - pemetrexed pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.0003 - chloro-2'-deoxyuridine L1210 parental enzyme 485427 2.1.1.45 0.000348 - nolatrexed pH 7.4, 25°C, recombinant enzyme 743569 2.1.1.45 0.0006 - pteroyltetraglutamate - 485395 2.1.1.45 0.0007 - 10-formyldihydropteroylheptaglutamate - 485398 2.1.1.45 0.0008 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.000833 - trimethoprim 1.0 mM 485404 2.1.1.45 0.00087 - trimethoprim 2.0 mM 485404 2.1.1.45 0.001 - pteroylpentaglutamate - 485395 2.1.1.45 0.001 - thymidine phosphate 0.25 mM, noncompetitive inhibition, 5,10-mehylenetetrahydrofolate as variable substrate 485404 2.1.1.45 0.0011 - 5-fluoro-2'-deoxyuridine-5'-monophosphate wild type enzyme, in 50 mM TES buffer, 50 mM, MgCl2, 13 mM formalin, 2 mM EDTA, 0.15 mM 2-mercaptoethanol, pH 7.4, at 25°C 720965 2.1.1.45 0.00124 - thymidine phosphate 1.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate 485404 2.1.1.45 0.0013 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.0013 - 2,4-diamino quinazoline - 485372 2.1.1.45 0.0013 - SK 28,757 - 485372 2.1.1.45 0.0014 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.0014 - dihydrofolate 1.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate 485404 2.1.1.45 0.0015 - bromo-2'-deoxyuridine L1210 parental enzyme 485427 2.1.1.45 0.0015 - SK 28,758 - 485372 2.1.1.45 0.0016 - 10-formyldihydropteroylpentaglutamate - 485398 2.1.1.45 0.0017 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.0017 - thiophosphate - 485430 2.1.1.45 0.00178 - dihydrofolate 5.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate 485404 2.1.1.45 0.00191 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.002 - 2-(4-hydroxy[1,1'-biphenyl]-3-yl)-4-methyl-1H-isoindole-1,3(2H)-dione pH not specified in the publication, temperature not specified in the publication 756644 2.1.1.45 0.002 - 5-fluoro-2'-deoxyuridylic acid - 485413 2.1.1.45 0.002 - pteroylhexaglutamate - 485395 2.1.1.45 0.0024 - 10-Formyltetrahydrofolylmonoglutamate - 485398 2.1.1.45 0.0027 - 1,3-propanediphosphonic acid pH 7.2, 22°C 690892 2.1.1.45 0.0029 - methasquin - 485372 2.1.1.45 0.0029 - SK 28,815 - 485372 2.1.1.45 0.00294 - dihydrofolate 0.5 mM, noncompetitive inhibition, dUMP as variable substrate 485404 2.1.1.45 0.003 - 2,4-diamino quinazoline antifolate - 485372 2.1.1.45 0.00303 - dihydrofolate 1.0 mM, noncompetitive inhibition, dUMP as variable substrate 485404 2.1.1.45 0.0034 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.0034 - Pteroylheptaglutamate - 485395 2.1.1.45 0.0034 - Pteroyltriglutamate - 485395 2.1.1.45 0.0037 - hydroxymethyl-2'-deoxyuridine L1210 parental enzyme 485427 2.1.1.45 0.0044 - quinaspar - 485372 2.1.1.45 0.00477 - 2',5-difluoro-ara-UMP - 702544 2.1.1.45 0.0049 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.0054 - 5-bromoacetamido-5'-deoxythymidine competitive inhibition 485391 2.1.1.45 0.0054 - 5-fluoro-2'-deoxyuridine-5'-monophosphate mutant enzyme E30W, in 50 mM TES buffer, 50 mM, MgCl2, 13 mM formalin, 2 mM EDTA, 0.15 mM 2-mercaptoethanol, pH 7.4, at 25°C 720965 2.1.1.45 0.0066 - 5-bromoacetamido-5'-deoxythymidine - 485391 2.1.1.45 0.0073 - thymidine phosphate L1210 parental enzyme 485427 2.1.1.45 0.00746 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.0075 - 10-formyldihydropteroylglutamate - 485398 2.1.1.45 0.0075 - deaza-aminopterin - 485372 2.1.1.45 0.0076 - pteroylmonoglutamate - 485395 2.1.1.45 0.00768 - iodo-2'-deoxyuridine L1210 parental enzyme 485427 2.1.1.45 0.0084 - dithiophosphate - 485430 2.1.1.45 0.0085 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.0093 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.01 - 5-bromo-2'-deoxyuridine 5'-monophosphate - 485384 2.1.1.45 0.0103 - 2'-fluoro-ara-UMP - 702544 2.1.1.45 0.013 - 2-[2-(3-methoxyphenoxy)propyl]-4-methyl-1H-isoindole-1,3(2H)-dione pH not specified in the publication, temperature not specified in the publication 756644 2.1.1.45 0.0132 - pteroyldiglutamate - 485395 2.1.1.45 0.015 - aminopterin - 485384 2.1.1.45 0.016 - 1-(2'-deoxyribosyl)-8-azapurin-2-one 5'-monophosphate - 485385 2.1.1.45 0.02 - 10-formyltetrahydropteroylmonoglutamate - 485398 2.1.1.45 0.02 - aminopterin - 485384 2.1.1.45 0.02 - methotrexate - 485384 2.1.1.45 0.022 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme 485427 2.1.1.45 0.023 - methopterin - 485393 2.1.1.45 0.023 - methotrexate uncompetitive with methylene tetrahydrofolate 485358 2.1.1.45 0.024 - 4,5,6,7-tetrachloro-2-[3-(phenylsulfanyl)propyl]-1H-isoindole-1,3(2H)-dione pH not specified in the publication, temperature not specified in the publication 756644 2.1.1.45 0.024 - dTMP - 485358, 485363 2.1.1.45 0.025 - 4'-[(4-methyl-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl][1,1'-biphenyl]-2-carbonitrile pH not specified in the publication, temperature not specified in the publication 756644 2.1.1.45 0.0284 - methopterin - 485372 2.1.1.45 0.03 - 2,4-diamino pteridine - 485372 2.1.1.45 0.0321 - 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme 485427 2.1.1.45 0.0347 - aminopterin - 485372 2.1.1.45 0.059 - dTMP - 485363 2.1.1.45 0.07 - dTMP variable substrate 2'-deoxyuridine 485393 2.1.1.45 0.073 - methopterin variable substrate 2'-deoxyuridine 485393 2.1.1.45 0.08 - thymidine phosphate - 485384 2.1.1.45 0.1 - dTMP - 485384 2.1.1.45 0.103 - methotrexate uncompetitive with dUMP 485389 2.1.1.45 0.12 - 1-(beta-D-2'-deoxyribofuranosyl)-1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate - 485385 2.1.1.45 0.12 - thymidine phosphate - 485384 2.1.1.45 0.14 - dTMP - 485363 2.1.1.45 0.238 - methotrexate 0.05 mM 485404 2.1.1.45 0.24 - dTMP variable substrate 5,10-methylenetetrahydropteroylglutamate 485393 2.1.1.45 0.267 - methotrexate 0.02 mM 485404 2.1.1.45 0.3125 - thymidine phosphate 0.25 mM, competitive inhibition, dUMP as variable substrate 485404 2.1.1.45 0.333 - thymidine phosphate - 485404 2.1.1.45 0.406 - methotrexate 0.5 mM 485404 2.1.1.45 0.413 - methotrexate 1.0 mM 485404 2.1.1.45 0.4328 - 2'-deoxy-2',2'-difluorouridine 5'-dihydrogen - 702544 2.1.1.45 0.6 0.9 pyridoxal 5'-phosphate - 485396 2.1.1.45 0.852 - trimethoprim - 485404 2.1.1.45 5 - aminofolate 1.0 mM 485404 2.1.1.45 5.2 - aminofolate 5.0 mM 485404 2.1.1.45 12 - glyceraldehyde 3-phosphate - 485399