Query String: SNX-482
Snx 5422 BDBM50514916
BDBM50450704 SNX-2112 CHEMBL560895
BDBM50480379 SNX-5422 CHEMBL553939
SNX-2112 CHEMBL560895 BDBM50378702
US10336717, Compound 482 BDBM113317 US8633212, 482 US9212153, 482
BDBM296747 US10112942, Example 482 US10172851, Example 482 US10137124, Example 482 US10953005, Example 482 US10555944, Example 482
US10881652, Example 482 US11648243, Example 482 BDBM305465 US10144734, Example 482 US10172845, Example 482 US10441581, Example 482
US10709712, Example 482 BDBM81183 US10245267, Example 482 US9694016, 482
US9745328, Compound 482 US9884878, Compound 482 BDBM169081 US9079866, 482
US9694002, 482 US9546164, 482 BDBM71440
US11014913, Example 482 US10870641, Example 482 US10550105, Example 482 BDBM431537
BDBM141055 US11547697, Compound 482 US9682141, 482
US10166249, Example 482 US9522888, 482 BDBM65126
BDBM137395 US20250017938, Compound 001-482 US8871790, 482
BDBM284472 US10023570, Example 482 US10174027, Example 482
BDBM486999 US11427601, Example 482 US10947252, Example 482
BDBM537953 US11603523, Example 482 US11248001, Example 482
US10710986, Example 482 BDBM452344 US11555029, No. 482
US10711020, Example 482 BDBM382771 US10273259, Example 482
US9938267, Cmpd ID 482 BDBM108901 US8604016, 482
US10730877, Example 482 BDBM428047 US11053244, Example 482 US10544143, Example 482 US10544143, Example 481
US10647713, Compound I-482 BDBM442521 US11396508, Compound I-482
US12221453, Compound I-482 BDBM565914 US11414431, Compound I-482
US20230279020, Example 482-1a BDBM440133 US10633389, Example 482-1a
US9751854, Compound I-482 US9802960, Compound I-482 BDBM338297
BDBM116765 US8637532, 482
BDBM120385 US8703785, 482
BDBM122043 US8722692, 482
BDBM130335 US8815840, 482
BDBM135000 US8846698, 482
BDBM137889 US8871934, 482
BDBM146562 US8957068, 482
BDBM157641 US9023865, 482
BDBM199846 US9226922, 482
BDBM206720 US9260425, 482
BDBM238795 US9394297, 482
BDBM47349 US9029559, 482
US8481536, 482 BDBM97917
US8846746, 482 BDBM133163
US9012443, 482 BDBM154427
US9034866, 482 BDBM159007
US9085555, 482 BDBM171052
US9120749, 482 BDBM177116
US9169252, 482 BDBM187939
US9260439, 482 BDBM207298
US9302989, 482 BDBM216601
US9328096, 482 BDBM226789
US9340517, 482 BDBM232094
US9434711, 482 BDBM248569
US9452986, 482 BDBM251178
US9458171, 482 BDBM253522
US9493446, 482 BDBM258013
US10071079, Example 480 US10478424, Example 482 US10071079, Example 482 BDBM273695
BDBM325276 US10189841, Compound I-482 US11161848, Compound I-482 1-(4-((2-(2- US10399980, Compound I-482
US10508120, Compound I-481 US11046698, Compound I-482 BDBM424026 US10508120, Compound I-482 US10577373, Compound I-482
BDBM269039 US9718825, Example 482
BDBM326896 US9662327, Compound 482
BDBM394834 US10307413, Compound 482
BDBM399005 US10323022, Example 482
BDBM410649 US10377770, Example 482
BDBM428048 US10544143, Example 482
BDBM454021 US10730863, Example 482
BDBM491499 US10975056, Example 482
BDBM525793 US11174252, Compound 482
BDBM538550 US11254663, Example 482
BDBM539135 US11254668, Example 482
BDBM561939 US11390631, Example 482
BDBM583590 US11524959, Compound 482.
BDBM584733 US11524968, Example 482
BDBM586484 US11530244, Compound 482
BDBM596885 US11596639, Example 482
BDBM635033 US11814367, Compound 482
BDBM666449 US20240116946, Example 482
BDBM677818 US20240174662, Example 482
BDBM681839 US20240199649, Compound 482
BDBM684079 US20240218021, Example 482
BDBM696884 US20240308985, Compound 482
BDBM732035 US12268694, Example 482
BDBM752216 US20250197382, Compound 482
BDBM759877 US20250236608, Example 482
BDBM762061 US12378224, Example 482
BDBM763437 US12384753, Example 482
US10071079, Example 482 BDBM273697
US10239843, Example 482 BDBM371374
US10266560, Example 482 BDBM379523
US11186582, Example 482 BDBM527446
US11261186, Example 482 BDBM540546
US11286268, Compound 482 BDBM544997
US11548892, Compound 482 BDBM588889
US11591336, Compound 482 BDBM596266
US11649255, Example 482 BDBM603509
US11685745, Example 482 BDBM607451
US11780845, Example 482 BDBM623463
US11834453, Example 482 BDBM638379
US11845723, Example 482 BDBM641586
US12319655, Example 482 BDBM746000
US20230279025, Example 482 BDBM617363
US20230348426, Example 482 BDBM632212
US20240025884, Example 482 BDBM647271
US20240043427, Example 482 BDBM650387
US20240246964, Compound 482 BDBM687461
US20240316047, Example 482 BDBM697701
US20250064789, Compound 482 BDBM723903
US20250145633, Example 482 BDBM739228
US8575197, I-482 BDBM105972
US8653087, III-482 BDBM117802
US9546153, ex. 482 BDBM210674
acs.jmedchem.1c00409_ST.482 BDBM512887
BDBM146355 US8957068, 481 US8957068, 482
BDBM321729 US10183021, Compound I-482
BDBM346847 US10202379, Reference Example 482
BDBM424027 US10508120, Compound I-482
BDBM441519 US10640495, Example I-482
BDBM555013 US11339144, Compound I-482
BDBM582469 US11518764, Compound I-482
BDBM606814 US11685732, Compound I-482
BDBM674171 US20240150321, Compound I-482
BDBM727621 US20250090540, Example I-482
US10144742, Compound I-482 BDBM306320
US10150728, Example I-482 BDBM307269
US10793563, Compound I-482 BDBM465144
US20250163057, Compound I-482 BDBM742208
US8614206, 482 US8614206, 483 BDBM110929
US9550763, Compound I-482 BDBM246808
US11130759, Cpd. No. 482 1-(2-chlorophenyl)-7-(difluoromethyl)- 4-(methylamino)quinazolin-2(1H)-one BDBM508172 US11084798, Cpd No 482 US11046691, Compound 482
BDBM158396 US10118915, Compound 486 US9682966, 482
BDBM674497 US20240150396, Compound 44 LL-482
BDBM674500 US20240150396, Compound 47 LL-482
BDBM547209 US11292791, Example 482 US11292791, Example 678
BDBM564168 Roche-Dataset for PDE10A, Compound 482
BDBM586483 US11530244, Compound 481 US11530244, Compound 482
BDBM714281 US20250025443, Example 315 US20250025443, Compound 482
BDBM714447 US20250025443, Compound 488 US20250025443, Example 482
US11001575, Example 483 US10457669, Example 482 BDBM417836
US9212182, 483 US9212182, 484 BDBM217402 US9212182, 482
US12012467, Compound DI-482 US12012467, Example 212 BDBM680998
US10233173, Example 482 US10071988, Example 482 BDBM276542 5-Chloro-2-[[1-(4-fluoro-3-methyl-phenyl)triazol-4-yl]methoxy]-4-
US11319329, Ex # 482 BDBM485638 N-((1R,2S)-2-Acrylamidocyclopentyl)-5-(2-methyl-4-(pyrimidin-5- yloxy)phenyl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8- triazaacenaphthylene-2-carboxamide US10934310, Ex # 482 US12065446, Example 482
BDBM606812 US11685732, Compound I-480 US11685732, Compound I-482
US10617676, Example 482 2-[[6-(4-Chlorophenyl)-2-oxo-3H-imidazo[4,5-b]pyridin-1- yl]methyl]benzonitrile US11207298, Example 482 BDBM437145
US9663496, Compound 482 N-(1-(4- cyanobenzyl)piperidin-4- yl)-6-(4-(4- methoxybenzoyl) piperidine-1-carbonyl)- N-methylnicotinamide US10377742, Compound 482 BDBM328344
Omnicef Cefzon CI-983 BDBM50248190 Cefdinir CHEBI:3485 FK-482
US10221163, Example 482 BDBM361325 N1-(2-(-2-amineoethylamino)ethyl)-4-(6-aminopyridin-3-yl)-3-(2H-tetrazol-5-yl)benzene-1,2-disulfonamide US10544130, Example 482
US11078201, Compound I-482 US11548890, Compound I-482 BDBM500817 US11021481, Compound I-482 7-[[5-[(2R)-2-[(3- fluoroazetidin- 1-yl)methyl]mor pholin-4-yl]-2- pyridyl]amino] 4-(7-fluoroimidazo [1,2-a]pyridin- 3-yl)isoindolin- 1-one
US11312688, Example 482 BDBM322133 US10183913, Example 482 1-{5-[(5-Chloro-2-fluorobenzyl)oxy]-1-(3-fluoro-3-methylbutyl)-1H-pyrazol-3-yl}-N-methylmethanamine hydrochloride
US10246456, Example 482 US10577367, Example 482 (S)-(6-(6-(6-(1-aminopropyl)pyridin-2-yl)-4-(2-methoxyethoxy)-1H-indazol-1-yl)pyrazin-2-yl)methanol BDBM374330
2-(((S)-3,3-difluoro-1-formylpiperidin-4-yl)oxy)-5-(4-((4-(S-methylsulfonimidoyl)phenyl)amino)-1,3,5-triazin-2-yl)benzonitrile US10253019, Example 482 US10040781, Example 482 BDBM278260
2-(5-cyclopropyl-3- (4',6-difluoro-[1,1'- biphenyl]-3-yl)-4-(4- sulfamoylbenzyl)- 1H-pyrazol-1- yl)thiazole-4- carboxylic acid; US10961200, Compound 482 BDBM489101 US11247971, Cmpd ID 482
BDBM486272 US10941160, Example 482 N-[5-[3-(methanesulfonamido)phenyl]- methyl-2-oxopyridin-3-yl]acetamide
US10344025, Example 482 BDBM405138 5-{3-fluoro-4-[4-({[5- (trifluoromethyl)pyridin-3- yl]methyl}carbamoyl)-1H-1,2,3- triazol-1-yl]butyl}-N-{[3- (trifluoromethoxy)phenyl]methyl}- 1,3,4-thiadiazole-2-carboxamide US11370786, Example 482
1-(3-Fluoroazetidin-1-yl)-2-(3-fluoro-6-phenyl-pyrrolo[3,2- BDBM409616 US10377753, Example 482
BDBM285428 N-[5-[3-(methanesulfonamido)phenyl]-1- methyl-2-oxopyridin-3-yl]acetamide US10023592, Example 482
US11014911, Example 481 BDBM498656 US11718603, Example 482 (1R,3S)-3-(3-{[(2-methyl-1,3- thiazol-5-yl)acetyl]amino}-1H- pyrazol-5-yl)cyclopentyl [3$#958;)- 3-methyltetrahydrofuran-3- yl]carbamate - Isomer A US11014911, Example 482
US11452717, Example 482 1-((1H-Pyrazol-4-yl)methyl)-3-(4-(pyrimidin-5-ylsulfonyl)phenyl)urea BDBM572880
(E)-N-((1r,4r)-4-(3-aminopropanamido)cyclohexyl)-3-(1H-imidazol-4-yl)acrylamide US10266526, Compound 482 BDBM378351
4-(3-Sulfamoyl-2-(1H-tetrazol-5-yl)-4-(trifluoromethyl)phenyl)benzo[d]thiazole-2-carboximidamide BDBM262630 US9708336, 482
BDBM443894 2-(2-ethyl-5-fluoropyridin-4-yl)-3-isopropyl-5-(piperidin-4-yl)-1H-indole US10660877, Example 482
N-(3,4-difluorophenyl)-1-[(1,3-dimethyl-1H-pyrazol-5-yl)sulfonyl]-4-phenylpyrrolidin-3-amine BDBM308963 US9656955, Example 482
BDBM512121 (1R,3S,5R)-2-(2-(3- acetyl-6-fluoro-5-(2- methylpyrimidin-5- yl)-1H-indol-1- yl)acetyl)-N-(6- bromo-3- methylpyridin-2-yl)-5- methyl-2- azabicyclo[3.1.0]hexane- 3-carboxamide US11084800, Cpd No. 482 US11708351, Compound 482
BDBM291026 (S)-2-(2-amino-2-cyclopropylethylamino)-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxamide US9579320, Example 482
US10005739, Example 482 BDBM401148 4-Ethylsulfonyl-3-[[4-oxo-7-(piperazin-1-ylmethyl)-6-(trifluoromethyl)quinazolin-3-yl]methyl]benzonitrile
US20250171431, Compound 482 2-{6-[3-(difluoromethyl)-1- piperazinyl]-5-methoxy-3- pyridylamino}-4-(6,7-difluoro-3- quinolylamino)pyrimidine BDBM745165
US9796708, Example 482 BDBM353250 4-(4-butoxy-3-fluorophenyl)-2-[1-(methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1H-pyrrolo[2,3-b]pyridine
BDBM355391 2-(4-methoxybenzyl)-6-oxo-N- {(1R)-1-[4-(pentafluoro-lambda6- sulfanyl)phenyl]propyl}-1,6- dihydropyrimidine-4-carboxamide US9815796, Example 482
N-(2-(1-methylazetidin-3- yl)-9H-xanthen-9-yl)-2-oxo- 6-(trifluoromethyl)-1,2- dihydropyridine-3- carboxamide BDBM667472 US11957687, Compound 482
US10577363, Compound 482 5-cyclopropyl-N-((2S,4S)-2-methyl-1- ((tetrahydrofuran-3-yl)sulfonyl)piperidin- 4-yl)isoxazole-3-carboxamide BDBM432782
BDBM654869 2,2-bis(hydroxymethyl)-6-[3-(pyridin- 4-yl)-1,2,4-oxadiazol-5-yl]-3,4- dihydro-2H-1-benzopyran-4-one US11912693, Compound 482
US10173991, Example 482 N-[(cyclopropyl- carbamoyl) methyl]-2-[6-(2- fluoropyridin-3- yl)-1,3- benzothiazol-2- yl]-2- (morpholine-4- sulfonyl)acetamide BDBM319431
US11028090, Example 482 BDBM502560 1- cyclohexyl- 3-[4-(7- methoxy-1- methyl-8- trifluoromethyl- [1,2,4]triazolo[4,3- a]quinoxaline- 4-ylamino)- butyl]-urea
US20250163063, Example 482 (3R,4S)-4-((7-cyclopentyl-5- fluoropyrrolo[2,1-f][1,2,4]triazin-2- yl)amino)tetrahydro-2H-thiopyran-3- ol BDBM742959
BDBM415369 US10428044, Example 482 Preparation of 3-{[2-(hydroxymethyl)-4-methylphenyl]amino}-6,6-dimethyl-2-(pyridin-4-yl)-1,5,6,7-tetrahydro-4H-indol-4-one
BDBM691093 US12065436, Compound 482 5-(5-ethyl-1,2,4-oxadiazol-3-yl)-N-(1- methyl-1H-pyrazol-4-yl)-2,3-dihydro- 1H-indene-1-carboxamide
US10336762, Compound 482 BDBM407540 4-((4-acetamido- bicyclo[2.2.2]octan-1- yl)amino)-6-(3-cyano- pyrrolo[1,2-b]pyridazin-7- yl)-N-methylnicotinamide
US12011444, Example 482 BDBM680267 4-{6-[2-(7-Cyano-4-fluoro-2-methyl-indol-1-yl)-ethylamino]-pyrimidin-4-yl}-2-isobutyl- benzoic acid
BDBM294926 2-(4,6-Dimethylpyrimidin-2-yl)-5-{[2-fluoro-6-(1-methyl-1H-imidazol-4-yl)phenyl]carbonyl}octahydropyrrolo[3,4-c]pyrrole US9586962, Example 482
US11839613, Example 482 BDBM640339 rac-2-(4 -{6-[2-(4-Fluoro-benzo[b]thiophen-5-yl)-ethylamino]- pyrimidin-4-yl}-2-propyl-phenyl)-propionic acid
US11802111, Example 482 ((1s,3s)-3-Hydroxy-3-methylcyclobutyl)(2-((6-methyl-5-(trifluoromethyl)pyridin-2-yl)oxy)-7-azaspiro[3.5]nonan-7-yl)methanone BDBM630892
BDBM274904 3-(2-(2- Fluoroisonicotinamido) imidazo[1,2- b]pyridazin-6-yl)-2- (4-fluorophenyl)-N- isopropyl-5,6- dihydroimidazo[1,2- a]pyrazine- 7(8H)-carboxamide US9556179, Compound 482
US10065972, Example 482 (R)-N-benzyl-1-[5-(2-fluoropropan-2-yl)-7-oxo-6,7-dihydro[1,3]thiazolo[5,4-d]pyrimidin-2-yl]pyrrolidine-2-carboxamide BDBM273129
6-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-N-[1-(cyclopropylmethyl)-3-(4-methoxyphenyl)-4-methyl-1H-pyrazol-5-yl]pyrimidin-4-amine BDBM531849 US11208400, Example 482
BDBM422578 3-[(1S)-1-(2-butyl-6- hydroxy-5-{[5-(2- methy!phenyl)pyridin-2- yl]sulfonyl}-4-oxo-1,4- dihydropyrimidin-1- yl)propyl]benzonitrile US10508104, Example 482
BDBM537658 N-ethyl-3-((1s,4s)-4-(2- fluorophenoxy)cyclohexyl)- 1-(4-((4-methylpiperazin-1- yl)methyl)phenyl)-1H- pyrazolo[3,4-c]pyridin-5- amine US11247990, Example 482
3-methyl- N-(2-{5-[5- (trifluoro- methyl)- 1,2,4-oxa- diazol-3- yl]pyridin- 2-yl}-1-[3- (trifluoro- methyl) phenyl] ethyl) oxetane-3- carboxamide US11066396, Example 482 BDBM505086
BDBM679040 US11998539, Example 482 (rac)-1-methyl-4- [4-(5-methyl-1,3- benzoxazol-2- yl)piperidin-1-yl]- 2-oxo-7-[(oxolan- 3-yl)oxy]-1,2- dihydroquinoline- 3-carboxamide
US10214537, Example 482 BDBM358412 4-acetyl-1-{3-[4-amino-5-(3-methyl- 1,2-oxazol-5-yl)pyrrolo[2,1-f][1,2,4] triazin-7-yl]phenyl}-3,3- dimethylpiperazin-2-one
(R)-2-(6-(sec-butylamino)-4-(3-((4- methyl-4H-1,2,4-triazol-3- yl)methyl)oxetan-3-yl)pyridin-2-yl)-4- (trifluoromethyl)isoindolin-1-one US20250230147, Compound 482 BDBM758301
(S)-8-chloro-6-(((6- fluoro-2-methylpyridin-3- yl)(1-(1-(hydroxymethyl)cyclopropyl)-1H- 1,2,3-triazol-4-yl)methyl)amino)-4- (neopentylamino)quinoline-3-carbonitrile US11066414, Compound 482 BDBM505833
3-((S)-3-((R)-8-(6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-ylsulfonyl)-1-oxa-8-azaspiro[4.5]decan-3-ylamino)-2-hydroxypropoxy)-N-methylbenzenesulfonamide US11987588, Compound 482 BDBM676013
BDBM300101 4-(benzyloxy)-N- [(2R)-1- hydroxypropan-2- yl]-6-[4-(4- methoxy-1H- pyrazolo[3,4- b]pyridin-3- yl)piperidin-1-yl]- 1,3,5-triazine-2- carboxamide US9593097, Example 482
BDBM498657 (1R,3S)-3-(3-{[(2-methyl-1,3- thiazol-5-yl)acetyl]amino}-1H- pyrazol-5-yl)cyclopentyl [3$#958;)- 3-methyltetrahydrofuran-3- yl]carbamate - Isomer B US11014911, Example 482
BDBM760734 N-[3-fluoro-4-[[6-methoxy-7-(2- methoxyethoxy)-1,5-naphthyridin-4- yl]oxy]phenyl]-5-(4-fluorophenyl)-4- hydroxy-2-(methoxymethyl)-6- methylpyridine-3-carboxamide US12371428, Compound 482
US10800792, Example 482 BDBM467821 N-((3R,5S)-1-Acryloyl-5-methoxypiperidin-3-yl)-5-(*S)-(2-methyl- 4-phenoxyphenyl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8- triazaacenaphthylene-2-carboxamide;
(8-morpholino-5,11-dihydro-6H- benzo[b]pyrido[2,3- e][1,4]diazepin-6-yl)((2R,5S)-5- ((1- (trifluoromethyl)cyclopropyl) amino)tetrahydro-2H-pyran-2- yl]methanone BDBM416338 US10442819, Example 482
2'-chloro-5'-methoxy-6-methyl-N-(5- (pyrazolo[1,5-a]pyrimidine-7-carbonyl)- 5,6-dihydro-4H-pyrrolo[3,4-d]thiazol-2- yl)-[4,4'-bipyridine]-3-carboxamide BDBM759030 US20250230171, Compound 482
US12187709, Compound 482 BDBM711123 6-((((2,2- difluorocyclopropyl)methyl)amino)methyl)- 2-(3-((1r,3r)-3-methoxy-1-(4-methyl-4H- 1,2,4-triazol-3-yl)cyclobutyl)phenyl)-4- (trifluoromethyl)isoindolin-1-one
4-(8-amino-3-{(3R)-1-[(3-methyloxetan-3-yl)carbonyl]piperidin-3-yl}imidazo[1,5-a]pyrazin-1-yl)-3-fluoro-N-(4-propoxypyridin-2-yl)benzamide US9718828, Example, 482 BDBM267869
US11319299, Example 482 BDBM553407 N-(cyclopropylmethyl)-2- [2-fluoro-5-[[6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carbonyl] amino]-4-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-1,3-thiazole-4- carboxamide
BDBM660045 (S,E)-3-(3-(3-Cyanopyrrolidin-1-yl)-3-oxoprop-1-en-1-yl)-N-cyclopropyl-7-hydroxy-4-isobutyl-5-oxo-4,5-dihydropyrazolo[1,5-a]pyrimidine-6-carboxamide US20240092784, Example 482
US20240109917, Example 482 2-(5,6-dihydro-4H- pyrrolo[1,2-b]pyrazol-3-yl)- N-(5-((2-(3,3- dimethylazetidin-1- yl)ethyl)carbamoyl)-2- methylpyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide BDBM664399
BDBM663644 US20240109900, Example 482 ((1R,5S,6r)-6-(4-methylthiazol-2-yl)-3-(3- (pyrazolo[1,5-a]pyridin-4-yl)-1H-pyrazolo[3,4- b]pyrazin-6-yl)-3-azabicyclo[3.1.0]hexan-6- yl)methanamine
US20240150293, Example 482 (1r,2′S,4S)-4-(3-chloroanilino)-2′-{3-[(2-methyl-1H-indol-4-yl)oxy]propyl}-2′,3′-dihydrospiro[cyclohexane-1,1′-indene]-4-carboxylic acid BDBM673335
(1R,3S,5R)-2-(2- (3-acetyl-5-(2- methylpyrimidin- 5-yl)-1H-indazol- 1-yl)acetyl)-N-(2- fluoro-3- methylbut-2-en-1- yl)-2- azabicyclo[3.1.0] hexane-3- carboxamide BDBM386542 US10287301, Compound 482
5-{4-amino-5-[(3- aminoazetidin-1- yl)methyl]pyrrolo[2,1- f][1,2,4]triazin-7- yl}-N[(3R,4S)-4- fluoro-1-(3,3,3- trifluoro-2- hydroxypropyl) pyrrolidin-3-yl]-2- methoxypyridine-3- carboxamide US11618753, Example 482 BDBM599339
US10822352, Comp No. 482 BDBM472208 (1R,3S,5R)-2-(2- (3-acetyl-5-(2- methylpyrimidin- 5-yl)-1H-indazol- 1-yl)acetyl)-N-(2- fluoro-3- methylbut-2-en-1- yl)-2-azabicyclo[3.1.0] hexane-3-carboxamide
(3S,6R,9S,18S,21S,25R,28S,34S)-9-benzyl-3-[2-[3-chloro-4-(trifluoromethyl)phenyl]ethyl]-28-cyclopentyl-6,7,10,13,16,21,22,25,29-nonamethyl-18-[(1S)-1-methylpropyl]spiro[1,4,7,10,13,16,19,22,26,29,32-undecazabicyclo[32.3.0]heptatriacontane-31,1'-cyclopentane]-2,5,8,11,14,17,20,23,27,30,33-undecone US20240148821, Compound 482 BDBM671438
6-(6-Aminopyridin-3-yl)-3-(2-methyl-5- (methylsulfonyl)phenyl)imidazo[1,2-a]pyrazin-8-amine BDBM421352 US10479795, Example 482 6-(6-Aminopyridin-3-yl)-3-(2-methyl-5- (methylsulfonyl)phenyl)imidazo[1,2-a]pyrazin-8-amine trifluoroacetate
BDBM630182 US20230340011, Example 482. (R)-4-((3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-1-(4-(5-methyl-1,3,4-oxadiazol-2-yl)piperazin-1-yl)pentan-1-one
US12310975, Example 482 BDBM743935 2-{[6-({5-chloro-2-[4-(1- {4-[2-(2,6- dioxopiperidin-3-yl)-1,3- dioxo-2,3-dihydro-1H- isoindol-5-yl]piperidin-1- yl}cyclopropyl)piperidin- 1-yl]pyrimidin-4- yl}amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl]oxy}-N- methylacetamide
- ChEMBL_1590573 (CHEMBL3829042) Inhibition of human recombinant HDAC1 (482 residues) by Color-de-Lys assay
- ChEMBL_2431056 Inhibition of PDE7A (130 to 482 residues) (unknown origin) using 3H-cAMP as substrate
- ChEMBL_1854477 (CHEMBL4355206) Inhibition of PDE7A1 catalytic domain (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21 cells
- ChEMBL_2187511 (CHEMBL5099593) Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells
- ChEMBL_2102822 (CHEMBL4811325) Inhibition of human HDAC1 (1 to 482 reidue) expressed in sf9 cells using Fluor de Lys as substrate by fluorimetric method
- ChEMBL_2150034 (CHEMBL5034496) Inhibition of PDE7A1 (130 to 482 residues) (unknown origin) using [3H]-cAMP substrate measured for 15 mins by liquid scintillation counting method
- ChEMBL_2313918 Inhibition of PDE7A (130 to 482 residues) (unknown origin) using 3H-cAMP as substrate incubated for 15 mins by liquid scintillation counter analysis
- ChEMBL_2172730 (CHEMBL5057864) Inhibition of TEV cleavage site fused N-terminal 6His-tagged PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli Rosetta2 (DE3)
- ChEMBL_1884229 (CHEMBL4385811) Inhibition of PDE7A1 catalytic domain (130 to 482 residues) (unknown origin) using [3H]-cAMP as substrate after 15 mins by liquid scintillation counting method
- ChEMBL_2073708 (CHEMBL4729242) Inhibition of PDE7A1 catalytic domain (130 to 482 residues) (unknown origin) using [3H]-cAMP as substrate after 15 mins by liquid scintillation counting method
- ChEMBL_2267271 Inhibition of human GST-tagged LSD1/CoREST (305 to 482 residues) expressed in Escherichia coli using pLys4Met peptide as substrate by UV-visible spectrophotometric analysis
- ChEMBL_874724 (CHEMBL2187957) Binding affinity to PDE7A1 catalytic domain (130 to 482 amino acid residues) using [3H]cGMP as substrate after 15 mins by liquid scintillation counter
- ChEMBL_1980012 (CHEMBL4613147) Inhibition of PDE7A1 (130 to 482 residues) (unknown origin) using [3H]-cAMP substrate incubated for 15 mins by liquid scintillation counting method relative to control
- ChEMBL_2090266 (CHEMBL4771529) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate
- ChEMBL_2172723 (CHEMBL5057857) Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay
- ChEBML_1726225 Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay
- ChEMBL_2051529 (CHEMBL4706228) Inhibition of PDE7A1 (130-482 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cAMP substrate incubated for 15 mins by liquid scintillation counting method
- ChEMBL_1669888 (CHEMBL4019776) Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate after 3 hrs by fluorescence assay
- ChEMBL_1726225 (CHEMBL4141503) Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay
- ChEMBL_2254407 (CHEMBL5168617) Inhibition of PDE7A1 (130-482 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counter method
- ChEMBL_2328971 Inhibition of recombinant PDE7A1 (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation method
- ChEMBL_1495533 (CHEMBL3580079) Inhibition of recombinant full length human HDAC1 (1 to 482) expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay
- ChEMBL_1765666 (CHEMBL4200913) Inhibition of PDE7A1 catalytic domain (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21 using 3H-cAMP as substrate after 15 mins by liquid scintillation counting
- ChEMBL_2124144 (CHEMBL4833377) Inhibition of PDE7A1 (130-482) (unknown origin) expressed in Escherichia coli BL21 assessed as using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counting analysis
- ChEMBL_2199361 (CHEMBL5111877) Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells incubated for 2 hrs by Multimode microplate reader analysis
- ChEMBL_2491696 Inhibition of recombinant PDE7A1 (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation method
- ChEBML_1681025 Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells using RHKKAc as substrate in presence of ATP
- ChEMBL_1728625 (CHEMBL4143903) Inhibition of recombinant human C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate by fluorescence assay
- ChEMBL_1800456 (CHEMBL4272748) Inhibition of N-terminal His-tagged human ARTD7 (482 to 678 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 3 hrs in presence of NAD+
- ChEMBL_1985254 (CHEMBL4618660) Inhibition of N-terminal His-tagged human ARTD7 (482 to 678 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 3 hrs in presence of NAD+
- ChEMBL_2146498 (CHEMBL5030844) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay
- ChEBML_1664374 Inhibition of PDE7A1 (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]cGMP or [3H]cAMP as substrate after 15 mins by liquid scintillation counting method
- ChEMBL_1829480 (CHEMBL4329354) Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay
- ChEMBL_1902491 (CHEMBL4404713) Inhibition of human PDE7A1 (130 to 482 residues) expressed in Escherichia coli BL21 codon-plus cells using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation counting method
- ChEMBL_1744410 (CHEMBL4178920) Inhibition of recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay
- ChEMBL_2163876 (CHEMBL5048737) Inhibition of recombinant human full length C-terminal His/FLAG tagged HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
- ChEMBL_2243513 (CHEMBL5157723) Inhibition of recombinant human full-length C-terminal Flag-His6-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry
- ChEMBL_2245295 (CHEMBL5159505) Inhibition of PDE7A1 (130 to 482 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H-GMP] or [3H-AMP] as substrate incubated for 15 mins by liquid scintillation counting method
- ChEMBL_2441471 Inhibition of full length C-terminal 6his-tagged human recombinant HDAC1 (1 to 482 residues) preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based analysis
- ChEMBL_1922376 (CHEMBL4425332) Inhibition of recombinant human PDE7A1 catalytic domain (130 to 482 residues) expressed in Escherichia coli BL21-CodonPlus cells using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation counting method
- ChEMBL_2030959 (CHEMBL4685117) Inhibition of recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorimetry analysis
- ChEMBL_2299355 Inhibition of full length C-terminal His/FLAG tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using RHK-K(Ac)-AMC as substrate incubated for 2 hrs
- ChEBML_1572330 Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay
- ChEMBL_2078806 (CHEMBL4734597) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay
- ChEMBL_2308504 Inhibition of full-length recombinant human HDAC1 (1 to 482 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate incubated for 30 mins by fluorescence based assay
- ChEMBL_2323562 Inhibition of full-length recombinant human HDAC1 (1 to 482 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate incubated for 30 mins by fluorescence based analysis
- ChEMBL_1571067 (CHEMBL3794853) Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay
- ChEMBL_1875121 (CHEMBL4376410) Inhibition of recombinant full length human FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetric assay
- ChEMBL_1978443 (CHEMBL4611578) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells by using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay
- ChEMBL_2056174 (CHEMBL4711175) Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay
- ChEMBL_2200944 (CHEMBL5113652) Inhibition of C-terminal 6xHis/FLAG-tagged full-length recombinant human HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic substrate incubated for 30 mins by fluorescence based plate reader analysis
- ChEMBL_2490285 Inhibition of C-terminal 6xHis/FLAG-tagged full-length recombinant human HDAC1 (1 to 482 residues) extracted from Sf9 cells using ZMAL (ZLys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay
- ChEMBL_2031889 (CHEMBL4686047) Inhibition of recombinant human full-length C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay
- ChEMBL_2188086 (CHEMBL5100168) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis
- ChEMBL_1669855 (CHEMBL4019743) Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay
- ChEMBL_1854947 (CHEMBL4355676) Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay
- ChEMBL_1971343 (CHEMBL4604161) Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetric assay
- ChEMBL_2052183 (CHEMBL4707184) Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay
- ChEMBL_2102862 (CHEMBL4811365) Inhibition of human HDAC1 (1 to 482 reidue) expressed in sf9 cells using ZMAL(Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition and measured after 20 mins by fluorimetric method
- ChEMBL_2363501 Inhibition of full length C-terminal 6His/FLAG-tagged human recombinant HDAC1 (1 to 482 residues) purified as tubulin complex expressed in Sf9 cells using ZMAL as fluorogenic substrate incubated for 90 mins by microplate reader analysis
- ChEMBL_2444624 Inhibition of C-terminal his/FLAG-tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using ZMAL-(Z-Lys(Ac)-AMC as substrate measured for 90 mins by microplate reader analysis
- ChEMBL_2487299 Inhibition of C-terminal 6His/FLAG tagged full length human recombinant HDAC1 (1 to 482 residues) extracted from Sf9 cells using Z-Lys(Ac)-AMC as substrate measured after 90 mins by fluorescence based microplate reader analysis
- ChEMBL_2497026 Inhibition of full length C-terminal his6-tagged human recombinant HDAC1 (1 to 482 residues) expressed in Sf9 cells using fluorogenic Boc-Lys(Ac)-AMC as substrate incubated for 90 mins by Synergy H1 plate reader analysis
- ChEMBL_2054189 (CHEMBL4709190) Inhibition of human C-terminal Flag tagged HDAC1 (1 to 482 residues) expressed in SF9 cells using Ac-peptide substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by microplate reader method
- ChEMBL_2103084 (CHEMBL4811587) Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) as fluorogenic substrate incubated for 90 mins by fluorescence based assay
- ChEMBL_2185901 (CHEMBL5097983) Inhibition of full length recombinant human HDAC1 (1 to 482 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins
- ChEMBL_1893016 (CHEMBL4394937) Inhibition of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method
- ChEMBL_1919883 (CHEMBL4422728) Inhibition of recombinant human His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
- ChEMBL_2059009 (CHEMBL4714010) Inhibition of C-terminal His/Flag-tagged human HDAC1 (1 to 482 residues) expressed in Sf9 cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate and trypsin addition and further incubated for 60 mins
- ChEMBL_2200962 (CHEMBL5113670) Inhibition of His-tagged recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS-SIRT1 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence based assay
- ChEMBL_2354853 Inhibition of C-terminal 6His/FLAG-tagged human recombinant full-length HDAC1 (1 to 482(end) residues) using Boc-Lys-(Ac)-AMC as substrate incubated for 10 mins followed by substrate addition measured after 1 hr by fluorescence based analysis
- ChEMBL_2381350 Inhibition of C-terminal 6His tagged human recombinant full length HDAC1 (1 to 482 residues) using Z- Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins followed by trypsin addition and measured after 30 min by microplate reader analysis
- ChEMBL_2456846 Inhibition of C-terminal 6His-FLAG-tagged human recombinant HDAC1 (1 to 482 residues) expressed in Sf9 cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by plate reader analysis
- ChEMBL_2477386 Inhibition of C-terminal 6xHis-tagged full-length recombinant human HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using a fluorogenic substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence based assay
- ChEMBL_1634442 (CHEMBL3877340) Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay
- ChEMBL_1838676 (CHEMBL4338809) Inhibition of recombinant full length human HDAC1 (1 to 482 residues) expressed in baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorometric method
- ChEMBL_2090121 (CHEMBL4771384) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method
- ChEMBL_2119796 (CHEMBL4828943) Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by addition of substrate and trypsin measured by flourescence assay
- ChEMBL_2328669 Inhibition of recombinant human LSD1 (172 to 852 residues)/His-tagged human CoREST (286 to 482 residues) expressed in Escherichia coli BL21 (DE3) cells using ART(mK)QTARKSTGGKAPRKQLAGGK-Biotin as substrate assessed as increase in H3K4 methylation incubated for 40 mins
- ChEMBL_2497023 Inhibition of full length C-terminal his6-tagged human recombinant HDAC1 (1 to 482 residues) expressed in Sf9 cells using trypsin and Ac-peptide as substrate preincubated with compound for 15 mins followed by substrate addition and measured after 60 mins
- ChEMBL_2028875 (CHEMBL4683033) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
- ChEMBL_2031694 (CHEMBL4685852) Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
- ChEMBL_2104899 (CHEMBL4813402) Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release using fluorogenic HDAC substrate 3 measured every 5 mins by fluorescence based analysis
- ChEMBL_2240171 (CHEMBL5154067) Inhibition of recombinant full length C-terminal His/Flag-tagged human HDAC1 (1 to 482 residues) using Z-Lys(Ac)-AMC as substrate preincubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based microplate reader analysis
- ChEMBL_1902905 (CHEMBL4405127) Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay
- ChEMBL_2340971 Inhibition of C-terminal His/FLAG-tagged human full length recombinant HDAC1 (1 to 482 residues) expressed in Sf9 cells using Boc-Lys(acetyI)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 30 mins by fluorescence based analysis
- ChEMBL_2487301 Inhibition of C-terminal 6His/FLAG tagged full length human recombinant HDAC1 (1 to 482 residues) extracted from Sf9 cells using Z-Lys(Ac)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by fluorescence based microplate reader analysis
- ChEMBL_2059505 (CHEMBL4714506) Inhibition of recombinant human full-length C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 insect cells using RHKK(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay
- ChEMBL_2092783 (CHEMBL4774046) Inhibition of recombinant human N-terminal GST-tagged HDAC-10 (1 to 482 residues) expressed in baculovirus infected in Sf9 cells using Boc-Lys (q-Ac)-AMC as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
- ChEMBL_2359058 Inhibition of C-terminal 6His/FLAG tagged human recombinant HDAC1 (1 to 482 residues) purified as tubulin complex expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by microplate reader analysis
- ChEMBL_2427788 Inhibition of C-terminal 6XHis-tagged/FLAG-tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis
- ChEMBL_2105758 (CHEMBL4814433) Inhibition of N-terminal His-SUMO tagged human LSD1 (172 to 852 residues)/His-tagged CoREST (286 to 482 residues) expressed in Escherichia coli BL21 (DE3) using ART(mK)QTARKSTGGKAPRKQLAGGK-Biotin as substrate preincubated for 60 mins followed by substrate addition and measured after 15 mins by HTRF assay
- ChEMBL_1854944 (CHEMBL4355673) Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay
- Steady State Kinetics Steady state kinetics were performed on an Agilent 8453 diode array spectrophotometer in sodium phosphate buffer (50 mM, pH 7.2) and a 1 cm pathlength cuvette. Inhibitor kinetics were performed using nitrocefin (NCF) as a reporter substrate (Δε482 = 17400 M^−1cm^−1). Production formation from NCF hydrolysis at an initial concentration of 100 μM in the presence of 0.05 μg/mL BlaC was assessed at 482 nm over a period of 300 s.
- SOD Assay (Fluorimetric Analysis) SOD activity of the purified samples was determined by the SOD assay kit using (2-(4-iodophenyl)-3-(4nitrophenyl)-5-(2,4-disulphenyl)-2H-tetrazolium, monosodium salt) [WST] which is a colorimetric assay that monitors the rate of inhibition of WST to a water soluble formazan dye. Purified SOD from bovine brain (20 μl) was incubated (37°C, 20 min) with WST working solution (200 μl) and distilled water (20 μl) according to the Sigma Information Bulletin, 19160 after which SOD activity was determined from the absorbance at 450 nm. Spectrofluorimetry was used to analyse the interaction of amyloid peptides [Aβ25-37, Aβ29-33 and Aβ1-40] with SOD. The excitation wavelength was fixed at 295 nm, the wavelength at which tryptophan absorbs, and the emission wavelength was at 482 nm. The change in fluorescence of the solution was monitored as increasing concentrations of amyloid peptides (0-40 μM) were added to a reaction mixture of SOD (5.0 μl) in Tris-HCl buffer (pH 8.0, 50 mM) in a final volume of 300 μl.