CHEMBL291812 BDBM50058606 N-(cyclopentylmethyl)-N-hydroxyurea
CHEMBL301645 N-(cyclobutylmethyl)-N-hydroxyurea BDBM50058577
CHEMBL59298 N-(cyclohexylmethyl)-N-hydroxyurea BDBM50058565
CHEMBL60903 BDBM50058607 N-(cyclopropylmethyl)-N-hydroxyurea
1-(3,4-dichlorophenyl)-3-hydroxyurea BDBM50188774 CHEMBL213348
1-(4-phenoxyphenethyl)-3-hydroxyurea CHEMBL197921 BDBM50175781
CHEMBL58668 N-(2-furylmethyl)-N-hydroxyurea BDBM50058630
N-(1-cyclopropylethyl)-N-hydroxyurea CHEMBL60664 BDBM50058558
N-(3-furylmethyl)-N-hydroxyurea BDBM50058639 CHEMBL59387
hydroxyurea BDBM50017811 CHEMBL467 US10155732, Compound HU HU
N-(1-Benzo(b)thien-2-ylethyl)-N-hydroxyurea ZILEUTON N-[1-(benzo[b]thiophen-2-yl)ethyl]-N-hydroxyurea (+-)-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea BDBM50000541 CHEMBL93 1-[1-(1-benzothien-2-yl)ethyl]-1-hydroxyurea Leutrol Zyflo (TN)
BDBM50058572 CHEMBL58909 N-[1-(4-bromophenyl)ethyl]-N-hydroxyurea
CHEMBL291840 BDBM50058634 N-[1-(2-furyl)ethyl]-N-hydroxyurea
BDBM50058570 N-[(2,5-dimethyl-3-furyl)methyl]-N-hydroxyurea CHEMBL59863
N-{[2-(2-furyl)cyclopropyl]methyl}-N-hydroxyurea BDBM50058567 CHEMBL292959
N-{[2-(3-furyl)cyclopropyl]methyl}-N-hydroxyurea CHEMBL294092 BDBM50058579
BDBM50006808 A-69412 N-[1-(3-furyl)ethyl]-N-hydroxyurea CHEMBL292371
BDBM50058593 N-[1-(1-benzothien-3-yl)ethyl]-N-hydroxyurea CHEMBL301461
BDBM50169723 CHEMBL186886 N-{(4-tert-butylbenzyl)-N'-hydroxyurea}methyl)phenyl]methanesulfonamide
BDBM50281095 CHEMBL405188 N-[3-(1-benzothien-2-yl)cyclobutyl]-N-hydroxyurea
CHEMBL300779 BDBM50058548 N-[1-(5-benzylthien-2-yl)ethyl]-N-hydroxyurea
CHEMBL433639 N-(dibenzo[b,d]furan-4-ylmethyl)-N-hydroxyurea BDBM50058587
CHEMBL58180 N-[1-(1-benzofuran-2-yl)ethyl]-N-hydroxyurea BDBM50058557
CHEMBL58225 N-[1-(2,5-dimethylthien-3-yl)ethyl]-N-hydroxyurea BDBM50058576
CHEMBL58448 N-{1-[2-(3-furyl)cyclopropyl]ethyl}-N-hydroxyurea BDBM50058559
CHEMBL58950 BDBM50058546 N-[1-(2,5-dimethyl-3-furyl)ethyl]-N-hydroxyurea
CHEMBL59077 N-[1-(1,1'-biphenyl-4-yl)ethyl]-N-hydroxyurea BDBM50058644
CHEMBL61891 N-[1-(1,3-benzothiazol-2-yl)ethyl]-N-hydroxyurea BDBM50058542
N-[1-(2,2'-bithien-5-yl)ethyl]-N-hydroxyurea BDBM50058632 CHEMBL293141
N-[1-(5-butyl-2-furyl)ethyl]-N-hydroxyurea CHEMBL58078 BDBM50058556
N-{1-[2-(2-furyl)cyclopropyl]ethyl}-N-hydroxyurea BDBM50058588 CHEMBL62090
N-{1-[5-(ethoxymethyl)-2-furyl]ethyl}-N-hydroxyurea CHEMBL61889 BDBM50058532
N-{3-[3-(4-fluorophenoxy)phenyl]cyclobutyl}-N-hydroxyurea BDBM50281097 CHEMBL87994
N-{1-[5-(4-fluorophenoxy)furan-2-yl]ethyl}-N-hydroxyurea CHEMBL58664 N-{(2E)-3-[5-(4-fluorophenoxy)-2-furyl]-1-methylprop-2-enyl}-N-hydroxyurea BDBM50058643
N-{3-[5-(4-fluorophenoxy)furan-2-yl]prop-2-ynyl}-N-hydroxyurea N-{3-[5-(4-fluorophenoxy)-2-furyl]prop-2-ynyl}-N-hydroxyurea BDBM50029778 CHEMBL264717
BDBM50042505 CHEMBL118956 N-[(6-heptyl-2H-chromen-3-yl)methyl]-N-hydroxyurea
BDBM50058550 N-[3-(2-furyl)-1-methylprop-2-ynyl]-N-hydroxyurea CHEMBL58062
CHEMBL292037 N-[(2E)-3-(2-furyl)prop-2-enyl]-N-hydroxyurea BDBM50058649
CHEMBL292447 N-[3-(3-furyl)-1-methylprop-2-ynyl]-N-hydroxyurea BDBM50058611
CHEMBL331748 BDBM50042513 N-[(6-bromo-2H-chromen-3-yl)methyl]-N-hydroxyurea
N-(1-{5-[(benzyloxy)methyl]-2-furyl}ethyl)-N-hydroxyurea CHEMBL61888 BDBM50058533
N-[(2,6-diphenyl-2H-chromen-3-yl)methyl]-N-hydroxyurea CHEMBL120362 BDBM50042495
(R)-(+)-N-{3-[5-(4-fluorophenoxy)furan-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea N-{3-[5-(4-fluorophenoxy)-2-furyl]-1-methylprop-2-ynyl}-N-hydroxyurea(A-78773) N-{3-[5-(4-fluorophenoxy)furan-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea N-{3-[5-(4-fluorophenoxy)-2-furyl]-1-methylprop-2-ynyl}-N-hydroxyurea A-78773 BDBM50029775 CHEMBL59598 (S)-(-)-N-{3-[5-(4-fluorophenoxy)furan-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea
BDBM50058561 CHEMBL58785 N-[(2E)-3-(2-furyl)-1-methylprop-2-enyl]-N-hydroxyurea
BDBM50058582 CHEMBL61874 N-[1-(5-chloro-1-benzofuran-2-yl)ethyl]-N-hydroxyurea
BDBM50058650 CHEMBL58314 N-[1-(1-benzothien-2-yl)ethyl]-N'-benzyl-N-hydroxyurea
CHEMBL301866 BDBM50058540 N-[(2E)-3-(3-furyl)-1-methylprop-2-enyl]-N-hydroxyurea
CHEMBL57963 N-[1-(3-chloro-1-benzothien-2-yl)ethyl]-N-hydroxyurea BDBM50058549
CHEMBL58246 BDBM50058589 N-[(2E)-3-(2-furyl)-1-methylprop-2-enyl]-N-hydroxyurea
CHEMBL58336 N-[1-(1-benzothien-2-yl)ethyl]-N'-butyl-N-hydroxyurea BDBM50058612
CHEMBL61417 N-[1-(1-benzothien-2-yl)ethyl]-N'-ethyl-N-hydroxyurea BDBM50058591
N'-allyl-N-[1-(1-benzothien-2-yl)ethyl]-N-hydroxyurea BDBM50058648 CHEMBL294752
N-({5-[(4-chlorophenyl)thio]thien-2-yl}methyl)-N-hydroxyurea CHEMBL58021 BDBM50058544
N-[1-(1,1-dioxido-1-benzothien-2-yl)ethyl]-N-hydroxyurea BDBM50058616 CHEMBL58906
N-[1-(4-chloro-1-benzothien-2-yl)ethyl]-N-hydroxyurea CHEMBL58463 BDBM50058555
N-[1-(5-fluoro-1-benzothien-2-yl)ethyl]-N-hydroxyurea CHEMBL294190 BDBM50058599
N-[1-(7-chloro-1-benzothien-2-yl)ethyl]-N-hydroxyurea BDBM50058568 CHEMBL300783
N-{[6-(4-fluorophenoxy)-2H-chromen-3-yl]methyl}-N-hydroxyurea CHEMBL330889 BDBM50042509
BDBM50058627 CHEMBL60174 N-[3-(1-benzothien-2-yl)-1-methylprop-2-ynyl]-N-hydroxyurea
CHEMBL119499 BDBM50042496 N-[(2,2-dimethyl-6-phenyoxy-2H-chromen-3-yl)methyl]-N-hydroxyurea
CHEMBL41928 BDBM50100898 N-{2-[(4'-cyano-1,1'-biphenyl-4-yl)oxy]ethyl}-N'-hydroxyurea
CHEMBL58756 BDBM50058609 N-[1-(5-tert-butyl-1-benzothien-2-yl)ethyl]-N-hydroxyurea
N-{2-[(4'-cyano-1,1'-biphenyl-4-yl)oxy]ethyl}-N-hydroxyurea CHEMBL43026 BDBM50100910
1-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)ethyl)-1-hydroxyurea BDBM50056766 CHEMBL445386 N-[2-(1-(4-Chlorobenzoyl)-5-methoxy-2-methylindol-3-yl)-1-ethyl]-N-hydroxyurea
BDBM50058590 CHEMBL293743 N-{3-[3-(4-fluorophenoxy)phenyl]-1-methylprop-2-ynyl}-N-hydroxyurea Fenleuton
BDBM50281096 CHEMBL86676 N-{(2E)-3-[3-(4-fluorophenoxy)phenyl]-1-methylprop-2-enyl}-N-hydroxyurea
CHEMBL359455 N-{3-[5-(4-fluorobenzyl)thien-2-yl]prop-2-ynyl}-N-hydroxyurea BDBM50029776
N-{3-[5-(4-fluorophenoxy)-2-furyl]-1,1-dimethylprop-2-ynyl}-N-hydroxyurea BDBM50058614 CHEMBL62146
N-{[7-(4-fluorophenoxy)-2,3-dihydro-1-benzoxepin-4-yl]methyl}-N-hydroxyurea CHEMBL355979 BDBM50283977
BDBM50029779 CHEMBL144028 N-{3-[5-(4-fluorobenzyl)thien-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea
BDBM50058585 N-{2-[({(1E)-[5-(4-fluorophenoxy)-2-furyl]methylene}amino)oxy]ethyl}-N-hydroxyurea CHEMBL61583
N-{2-[({(1E)-[5-(4-fluorophenoxy)-2-furyl]methylene}amino)oxy]ethyl}-N-hydroxyurea BDBM50058635 CHEMBL60523
BDBM50280281 CHEMBL42593 N-{[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]methyl}-N-hydroxyurea
CHEMBL145306 BDBM50029777 (S)-(-)-N-{3-[5-(4-fluorobenzyl)thien-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea
N-{(2Z)-3-[5-(4-fluorophenoxy)furan-2-yl]-1-methylprop-2-enyl}-N-hydroxyurea CHEMBL145318 BDBM50029780
CHEMBL160218 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-hydroxyurea BDBM50286668
CHEMBL294028 N-{(2Z)-2-fluoro-3-[5-(4-fluorophenoxy)-2-furyl]-1-methylprop-2-enyl}-N-hydroxyurea BDBM50058554
CHEMBL307609 BDBM50144624 (5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-ylmethyl)-N-hydroxyurea
CHEMBL410500 BDBM50280279 N-{1-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]ethyl}-N-hydroxyurea
A-85761 (R)-(+)-N-{3-[5-(4-fluorobenzyl)thien-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea N-{(1R)-3-[5-(4-fluorobenzyl)thien-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea Atreleuton CHEMBL59356 N-{(1R)-3-[5-(4-fluorobenzyl)thien-2-yl]-1-methylprop-2-ynyl}-N-hydroxyurea (ABT-761) {3-[5-(4-Fluoro-benzyl)-thiophen-2-yl]-1-methyl-prop-2-ynyl}-hydroxy urea BDBM50029781
BDBM50144621 CHEMBL73148 CMI-977 N-(4-{(2S,5S)-5-[(4-fluorophenoxy)methyl]tetrahydrofuran-2-yl}but-3-ynyl)-N-hydroxyurea
BDBM50286662 CHEMBL160148 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-benzyl-N-hydroxyurea
BDBM50286666 CHEMBL347382 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-ethyl-N-hydroxyurea
BDBM50309614 1-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-3-hydroxyurea CHEMBL598868
CHEMBL155975 BDBM50286664 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-cyclohexyl-N-hydroxyurea
BDBM50076656 N-{1-methyl-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea CHEMBL173939
CHEMBL155851 BDBM50286667 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-(tert-butyl)-N-hydroxyurea
CHEMBL160290 BDBM50286661 N-hydroxy-N'-[3-methoxy-5-(5-(3,4,5-trimethoxyphenyl)tetrathydrofuran-2-yl)-2-propoxyphenyl]-N-(sec-butyl)-N-hydroxyurea
CHEMBL175150 N-{1-ethyl-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea BDBM50076644
CHEMBL366595 N-{1-isopropyl-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea BDBM50076653
CHEMBL73706 BDBM50144620 [4-(5-{4-[Bis-(4-fluoro-phenyl)-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-but-3-ynyl]-N-hydroxyurea
N-Hydroxy-N-[1,2,3,4-tetrahydro-6-(benzyloxy)-1-naphthalenyl]urea 1-(6-(benzyloxy)-1,2,3,4-tetrahydronaphthalen-1-yl)-1-hydroxyurea BDBM50055115 CHEMBL146240
N-{1-ethyl-3-[1-(4-methoxyphenyl)-5-(4-chlorophenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea BDBM50076652 CHEMBL262539
N-{1-isopropyl-3-[1-(4-methoxyphenyl)-5-(4-chlorophenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea CHEMBL176668 BDBM50076663
N-{1-methyl-3-[1-(4-methoxyphenyl)-5-(4-chlorophenyl)-1H-pyrazol-3-yl]prop-2-ynyl}-N-hydroxyurea BDBM50076649 CHEMBL369848
3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-cyclohexyl-1-hydroxyurea BDBM50309620 CHEMBL596623
BDBM50309616 CHEMBL603962 3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-ethyl-1-hydroxyurea
CHEMBL603907 3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-cyclopentyl-1-hydroxyurea BDBM50309619
1-tert-butyl-3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-hydroxyurea BDBM50309618 CHEMBL597236
BDBM50309621 CHEMBL599285 3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-(4,4-difluorocyclohexyl)-1-hydroxyurea
CHEMBL185825 BDBM50155339 1-{4-[4-(3-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}propoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea
CHEMBL187637 1-{4-[4-(2-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}ethoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea BDBM50155340
BDBM50144622 CHEMBL312082 [3-(5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-1-methyl-prop-2-ynyl]-N-hydroxyurea
BDBM50155333 CHEMBL425358 1-{4-[4-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea
BDBM50155338 1-{4-[4-(4-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}butoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea CHEMBL186125
CHEMBL187264 BDBM50155335 1-{4-[4-(3-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}propoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea
[4-((2S,5S)-5-{4-[Bis-(4-fluoro-phenyl)-methyl]-piperazin-1-ylmethyl}-tetrahydro-furan-2-yl)-but-3-ynyl]-N-hydroxyurea BDBM50144623 CHEMBL74779
BDBM50309622 3-((5'-chloro-3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1-(1,3-difluoropropan-2-yl)-1-hydroxyurea CHEMBL599490
BDBM662358 US20250241908, Compound A271 US20240109853, Compound A271 1-(4-(2-(4- chlorophenyl)but-3-yn- 2-yl)thiazol-2-yl)-3- hydroxyurea US20240226094, Compound A271
[4-((2R,5R)-5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-tetrahydro-furan-2-yl)-but-3-ynyl]-N-hydroxyurea CHEMBL74688 BDBM50144627
[4-((2S,5S)-5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-tetrahydro-furan-2-yl)-but-3-ynyl]-N-hydroxyurea CHEMBL305662 BDBM50144626
BDBM50155336 CHEMBL444083 1-{4-[4-(4-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}butoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea N-hydroxycarbamate derivative
BDBM50155334 CHEMBL360202 1-(4-{4-[4-(4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene}piperidin-1-yl)butoxy]phenyl}but-3-yn-1-yl)-1-hydroxyurea
CHEMBL185905 BDBM50155337 1-(4-{4-[2-(4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene}piperidin-1-yl)ethoxy]phenyl}but-3-yn-1-yl)-1-hydroxyurea
CHEMBL188021 BDBM50155341 1-(4-{4-[3-(4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene}piperidin-1-yl)propoxy]phenyl}but-3-yn-1-yl)-1-hydroxyurea
1-[4-(5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-but-3-ynyl]-N-hydroxy-urea CHEMBL73135 [4-(5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-but-3-ynyl]-N-hydroxyurea BDBM50144625
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- Exell, JC; Thompson, MJ; Finger, LD; Shaw, SJ; Debreczeni, J; Ward, TA; McWhirter, C; Siöberg, CL; Martinez Molina, D; Abbott, WM; Jones, CD; Nissink, JW; Durant, ST; Grasby, JA Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site. Nat Chem Biol 12: 815-21 (2016)
- Temperini, C; Innocenti, A; Scozzafava, A; Supuran, CT N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors. Bioorg Med Chem Lett 16: 4316-20 (2006)
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- Adams, JL; Garigipati, RS; Sorenson, M; Schmidt, SJ; Brian, WR; Newton, JF; Tyrrell, KA; Garver, E; Yodis, LA; Chabot-Fletcher, M; Tzimas, M; Webb, EF; Breton, JJ; Griswold, DE Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea. J Med Chem 39: 5035-46 (1997)
- ChEMBL_743386 (CHEMBL1767685) Inhibition of ATR in human HT-29 cells assessed as hydroxyurea-induced phosphorylation of H2AX by immunofluorescence microscopy
- ChEMBL_820801 (CHEMBL2038506) Inhibition of CHK1 in human U2OS cells pretreated with hydroxyurea assessed as gamma-H2AX level after 2 hrs by immunofluorescence assay
- ChEMBL_959662 (CHEMBL2382855) Inhibition of CHK1 in human U2OS cells assessed as phosphorylation of H2AX after 2 hrs by FITC/propidium iodide staining-based immunofluorescence assay in presence of hydroxyurea
- RNR Enzyme Activity Assay A rapid-fire mass spectrometry (RF/MS) assay was used to assess RNR enzyme activity using a 384 well plate and a robotic platform.[0402]The plate layout included two validated reference compounds (Triapine (3-AP) and Hydroxyurea (HU)):A dose response in duplicate; top concentration: 5 μM (3-AP) and 250 μM (HU), semi-logdilutions.Spike wells in triplicate randomly spotted at four concentrations:250 μM, 100 μM, 30 μM and 2 μM for HU5 μM, 2 μM, 0.6 μM and 0.04 μM for 3-APFirst, the multidrop pipes were saturated for 30 minutes with enzymatic solution. Then 30 μL of Stop solution was distributed in column 24. Next, 15 μL of enzyme was distributed in column 1 to 24. Next, a pre-incubation step of 15 minutes at room temperature occurred, followed by distribution of 15 μL of substrate solution (column 1 to 24). Next, the plate was incubated for 45 minutes at 37° C. 30 μL of Stop solution was distributed to columns 1 to 23.The final parameters for the enzyme reactions were:Incubation: 37° C., 45 min[CDP]: 5 μM; [ATP]: 1 mM; [NADPH]: No[RNR]final: 50 nM with 1:1 (RNR1:RNR2) ratioFinal volume: 30 μLStop solution: 6% HCOOH containing 2 μM of 15
- Rapid-Fire Mass Spectrometry (RFMS) Assay A rapid-fire mass spectrometry (RFMS) assay was used to assess RNR enzyme activity using a 384 well plate and a robotic platform. The plate layout included two validated reference compounds (Triapine (3-AP) and Hydroxyurea (HU)): A dose response in duplicate; top concentration: 5 uM (3-AP) and 250 uM (HU), semi-log dilutions. Spike wells in triplicate randomly spotted at four concentrations: 250 uM, 100 uM, 30 uM and 2 uM for HU 5 uM, 2 uM, 0.6 uM and 0.04 uM for 3-AP First, the multidrop pipes were saturated for 30 minutes with enzymatic solution. Then 30 uL of Stop solution was distributed in column 24. Next, 15 uL of enzyme was distributed in column 1 to 24. Next, a pre-incubation step of 15 minutes at room temperature occurred, followed by distribution of 15 uL of substrate solution (column 1 to 24). Next, the plate was incubated for 45 minutes at 37 C. 30 uL of Stop solution was distributed to columns 1 to 23. The final parameters for the enzyme reactions were: Incubation: 37 C., 45 min [CDP]: 5 uM; [ATP]: 1 mM; [NADPH]: No [RNR]final: 50 nM with 1:1 (RNR1:RNR2) ratio Final volume: 30 uL Stop solution: 6% HCOOH containing 2 uM of 15 The compounds were screened at concentrations from 10 nM to 30 uM.