PROTAC研发服务平台_药效筛选-尊龙凯时人生就博官网登录,ag尊龙凯时，尊龙凯时生物医药

PROTAC技术作用机制独特

1.PROTAC分子通过其一端的靶蛋白配体（POI Ligand）特异性识别并结合靶蛋白，通过其另一端的E3泛素连接酶配体（E3 Ligase Ligand）特异性识别并结合E3 Ligase；
2.形成P O I - P R O T A C - E3 ligase三元复合体；
3. 在此三元复合体中，靶蛋白POI被E3 ligase泛素化修饰，泛素化修饰了的POI随后被蛋白酶体识别并降解，由此抑制靶蛋白的功能。

PROTAC技术优势

改变靶点的“不可成药性”（undruggable）
PROTAC的作用分子机制是通过泛素-蛋白酶体系统降解靶蛋白，并非通过竞争结合以封闭靶蛋白功能区而发挥蛋白功能抑制作用，因此PROTAC对靶蛋白识别结合区不一定非得是活性区，结合力也不一定必须是高亲和力；这使得一些缺乏高亲和力小分子结合的“不可成药性”靶蛋白变成“可成药性”。
高效性
传统小分子抑制剂通过竞争结合靶蛋白活性功能域而抑制靶蛋白功能，所需小分子的量往往较大；而PROTAC通过泛素-蛋白酶体系统降解靶蛋白以解除靶蛋白功能，故具有可循环使用性、用量低和高效性的特点。
无免疫原性
与抗体药物相比，PROTAC不会引发抗药抗体产生。
综上，PROTAC已成为药物研发领域的新兴利器，在国内外备受科研单位及药企所追捧。

尊龙凯时人生就博官网登录,ag尊龙凯时，尊龙凯时PROTAC技术服务

靶标蛋白PROTAC-POI的设计合成
尊龙凯时人生就博官网登录,ag尊龙凯时，尊龙凯时汇总了当前流行的热门POI配体，不同组织类型的E3ligase配体，并且建立了含数百种连接分子的linker库。
此外，尊龙凯时人生就博官网登录,ag尊龙凯时，尊龙凯时成熟的计算机辅助药物设计技术平台，大大提高PROTAC-POI的设计合成质量。
PROTAC-POI的体外筛选
细胞增殖实验（CCK-8或MTT法）
通过细胞增殖实验检测作用机制。
检测HiBiT-IRAK4 过表达 OCI-LY10 细胞中 HiBiT-IRAK4 的降解百分比
Western Blot（WB检测法）
通过WB实验检测初筛到的PROTAC-POI分子对靶蛋白的降解能力，分析DC₅₀值。
Western Blot检测用 IRAK4 degrader-1理的 OCI-LY10 细胞
IRAK4 degrader-1 是一种基于 Pomalidomide 的CRBN型PROTAC
MG132抑制实验表明IRAK4 degrader-1通过蛋白酶体途径降解IRAK4
Tumor cell proliferation inhibition effect test
IRAK4 Degrader-1对OCI-LY10细胞的生长抑制作用
ACBI1（BRM 降解剂）以剂量依赖性方式降解 BRM蛋白

PROTAC-POI的动物体内药效筛选

CDX小鼠肿瘤模型

将相应癌种细胞系移植到裸鼠或NSG小鼠体内，建立皮下瘤或原位瘤模型，通过口服、灌胃或静脉给药，检测体外筛到的PROTAC-POI对鼠体内肿瘤生长的抑制效果。

Cancer Type	Orthotopic Model	Orthotopic Model (Luc Cell Line)
胶质母细胞瘤	U87-MG	U87-MG-luc
肺癌	NCI-H1650, A549, NCI-H1975, NCI-H460, LLC1	A549-luc, LLC1-luc,NCI-H1975-luc
结肠癌	HCT-116, LoVo	HT29-luc
胃癌	Hs 746T
胰腺癌	Mia-Paca 2	Mia-Paca 2-luc
乳腺癌	MDA-MB-231	4T1-luc
卵巢癌	SK-OV-3	SK-OV-3-luc
前列腺癌	PC3	PC-3-luc
肾癌	A498
膀胱癌	UM-UC-3
黑色素瘤		B16-F10-luc
肝癌	H22
骨癌

PDX小鼠肿瘤模型

将肿瘤组织以组织块的形式移植到NSG小鼠体内，这些肿瘤组织在NSG小鼠体内保持了原始肿瘤的生物学特征，与临床特征相似度更高。利用PDX小鼠模型检测PROTAC-POI对体内肿瘤生长的抑制效果。

癌症类型	细胞系
结肠癌	PDXM-008C, PDXM-016C, PDXM-020C, PDXM-021C, PDXM-057C, PDXM-060C, PDXM-075C, PDXM-076C, PDXM-087C, PDXM-104C, PDXM-095C, PDXM-084C, PDXM-072C, PDXM-069C, PDXM-057C, PDXM-015C, PDXM-002C,
肺癌	PDXM-054Lu, PDXM-050Lu, PDXM-047Lu, PDXM-053Lu, PDXM-028Lu,
胃癌	PDXM-092Ga, PDXM-091Ga,
乳腺癌	PDXM-201B, PDXM-202B, PDX-203B
肝癌	PDXM-211Li, PDXM-212Li
胰腺癌	PDXM-221Pa, PDXM-222Pa
膀胱癌	PDXM-231U, PDXM-232U
淋巴瘤	PDXM-241Ly, PDXM-242Ly

一站式临床前研究服务
PK/PD研究、药学分析、药物代谢动力学研究和安全性评价
对动物体内药效检测筛选得到的理想的PROTAC-POI进行PK/PD研究、药学分析、药物代谢动力学研究和安全性评价，并汇总实验结果和材料进行IND申报，以助力客户加快PROTAC-POI药物的研发进程。
五种高效雄激素受体 (AR) 降解剂在小鼠中静脉和口服给药的药代动力学 (PK) 数据，其中最优化合物为ARD-2128。PK 数据显示，ARD-2128具有出色的整体 PK 曲线：低清除率 (1.2 mL/min/kg) 和中高稳态分布容积 (V_ss为2.7 L/kg)。ARD-2128 按 2 mg/kg 剂量静脉给药后的 T_1/2为 27.6 小时，按 5 mg/kg 剂量口服给药后T_1/2 为 18.8 小时。ARD-2128 (5 mg/kg) 在小鼠体内达到 67% 的口服生物利用度，通过口服给药有效降低 AR 蛋白并抑制肿瘤组织中的 AR 调节基因，从而有效抑制小鼠肿瘤生长且无毒性迹象。
五种化合物在雄性 ICR 小鼠中的 PK 数据汇总^[1]
ARD-2128 在小鼠、大鼠、犬、猴和人五种属中的血浆稳定性。数据显示，ARD-2128 在所有五种属中都具有稳定的血浆稳定性。
ARD-2128 在五种属中的肝微粒体中代谢稳定性和血浆稳定性^[1]
参考文献：
[1].Xin Han,et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer.J Med Chem. 2021 Sep9;64(17):12831-12854. doi: 10.1021/acs.jmedchem.1c00882. Epub 2021 Aug 25.

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中间体

尊龙凯时人生就博官网登录,ag尊龙凯时，尊龙凯时中间体产品列表
Number	Compound Name	Purity	Inventory
1	4-(methoxycarbonyl)benzyl 1H-indole-4-carboxylate	88.91	5.5 g
2	4-(methoxycarbonyl)benzyl 1H-indazole-4-carboxylate	85.34	4.7 g
3	2-chloro-5-(4-fluorophenyl)thiazole-4-carbonitrile	97.97	2 g
4	2-(5-((3-((2H-tetrazol-5-yl)methoxy)azetidin-1-yl)sulfonyl)-2-ethoxyphenyl)-5-methyl-7-propyl-4a,7-dihydroimidazo[5,1-f][1,2,4]triazin-4(3H)-one	99.28	2 g
5	2-((1-((4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4,4a,7-tetrahydroimidazo[5,1-f][1,2,4]triazin-2-yl)phenyl)sulfonyl)azetidin-3-yl)oxy)acetonitrile	99.76	2 g
6	2-(5-((3-((1H-1,2,3-triazol-4-yl)methoxy)azetidin-1-yl)sulfonyl)-2-ethoxyphenyl)-5-methyl-7-propyl-4a,7-dihydroimidazo[5,1-f][1,2,4]triazin-4(3H)-one	98.86	4.5 g
7	2-(5-((3-aminoazetidin-1-yl)sulfonyl)-2-ethoxyphenyl)-5-methyl-7-propyl-4a,7-dihydroimidazo[5,1-f][1,2,4]triazin-4(3H)-one	98.98	1.5 g
8	methyl 4-(3-(4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)prop-1-yn-1-yl)-3-((2-methoxyethoxy)methyl)benzoate	96.43	0.5 g
9	methyl 4-(3-(4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)prop-1-yn-1-yl)-3-((4-methoxybutoxy)methyl)benzoate	96.73	0.46 g
10	4-(3-(4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)prop-1-yn-1-yl)-3-((2-methoxyethoxy)methyl)benzoic acid	97.16	0.03 g
11	methyl 4-(3-(4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)prop-1-yn-1-yl)-3-((3-methoxypropoxy)methyl)benzoate	95.65	0.05 g
12	4-((3-((4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)phenyl)sulfonamido)azetidin-1-yl)methyl)-3-fluoro-N-hydroxybenzamide	95.97	0.2 g
13	methyl 6-(((1-((4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)phenyl)sulfonyl)azetidin-3-yl)amino)methyl)nicotinate	\	0.44 g
14	4-(methoxycarbonyl)benzyl 1H-indole-6-carboxylate	97.47	1.6 g
15	4-(methoxycarbonyl)benzyl 1H-indazole-6-carboxylate	95.72	1.7 g
16	2-(5-((3-((2H-tetrazol-5-yl)methyl)-3-hydroxyazetidin-1-yl)sulfonyl)-2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one	96.12	6 g
17	2,2-dimethyl-4-nitrobutanoic acid	\	2.5 g
18	4-(methoxycarbonyl)benzyl 1H-indole-5-carboxylate	95.04	2.4 g
19	4-(methoxycarbonyl)benzyl 1H-indazole-5-carboxylate	70	3 g
20	2-(5-chloro-2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one	79.236	0.9 g
21	2-(2-ethoxy-5-iodophenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one	98.575	5.3 g
22	2-chloro-8-cyclopentyl-6-iodo-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one	94.943	2.2 g
23	N-(5-(4-aminobutyl)pyridin-2-yl)-5-fluoro-4-(4-methylpiperazin-1-yl)pyrimidin-2-amine	99.207	1.1 g
24	2-chloro-5-fluoro-4-(4-methylpiperazin-1-yl)pyrimidine	93.522	6.1 g
25	4-chloro-5-fluoro-N-(5-nitropyridin-2-yl)pyrimidin-2-amine	87.86	3.4 g
26	4-(3-(5-((4-(3-(dimethylamino)azetidin-1-yl)-5-fluoropyrimidin-2-yl)amino)pyridin-2-yl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile	100	0.12 g
27	4-(3-((5-((5-fluoro-4-(4-methylpiperazin-1-yl)pyrimidin-2-yl)amino)pyridin-2-yl)methyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile	90.453	0.1 g
28	methyl 4-(((1-((4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)phenyl)sulfonyl)azetidin-3-yl)amino)methyl)-3-fluorobenzoate	99.188	16 g
29	2-(5-bromo-2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one	97.927	1.9 g
30	2-(5-amino-2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one	85.65	33.4 g
31	methyl 1-(5-bromopyridin-2-yl)piperidine-4-carboxylate	100	16.2 g
32	3-(2-((3-(4-(ethoxycarbonyl)phenoxy)phenyl)amino)-2-oxoethyl)-1H-indole-2-carboxylic acid	90	310 mg
33	methyl 3'-nitro-[1,1'-biphenyl]-3-carboxylate	92	630 mg
34	3-(2-((3'-(1-methoxyvinyl)-[1,1'-biphenyl]-3-yl)amino)-2-oxoethyl)-1H-indole-2-carboxylic acid	93	270 mg
35	3-(2-((3-(2-(methoxycarbonyl)phenoxy)phenyl)amino)-2-oxoethyl)-1H-indole-2-carboxylic acid	92	150 mg
36	methyl 4,6-dichloropicolinate	100	120 mg
37	(R)-4-(5-chloropyrazolo[1,5-a]pyrimidin-7-yl)-3-methylmorpholine	100	120 mg
38	(S)-4-(3,6-dichloropyridazin-4-yl)-3-methylmorpholine	94	110 mg
39	3-(6-chloro-5-morpholinopyridazin-3-yl)-8-oxa-3-azabicyclo[3.2.1]octane	99	120 mg
40	5-chloro-7-(cyclopropylsulfonyl)pyrazolo[1,5-a]pyrimidine	98	110 mg
41	5-bromopyrazolo[1,5-a]pyridine	100	120 mg
42	(R)-4-(7-iodopyrazolo[1,5-a]pyrimidin-5-yl)-3-methylmorpholine	90	108 mg
43	4-bromo-3,6-dichloropyridazine	90	104 mg
44	(1R,5S)-3-(4-((R)-3-methylmorpholino)-7-(1H-pyrazol-3-yl)imidazo[1,5-b]pyridazin-2-yl)-8-oxa-3-azabicyclo[3.2.1]octane	85	111 mg
45	(1R,5S)-3-(pyrazolo[1,5-a]pyrimidin-5-yl)-8-oxa-3-azabicyclo[3.2.1]octane	95	108 mg
46	4-(3,6-dichloropyridazin-4-yl)-2-methylmorpholine	90	106 mg
47	N-((6-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-4-(2-methylmorpholino)pyridazin-3-yl)methyl)-1H-pyrazole-5-carboxamide	90	133 mg
48	8-chloro-2-morpholino-1,7-naphthyridin-4-ol	90	101 mg
49	3,6-dichloro-4-(piperidin-1-yl)pyridazine	95	105 mg
50	7-benzyl-3-chloroisoquinoline	95	102 mg
51	2-(2,6-dioxopiperidin-3-yl)-5-(4-(hydroxymethyl)piperidin-1-yl)isoindoline-1,3-dione	90	109 mg
52	3-(6-chloro-5-(3,3-dimethylmorpholino)pyridazin-3-yl)-8-oxa-3-azabicyclo[3.2.1]octane	90	133 mg
53	2-(2,6-dioxopiperidin-3-yl)-5-(3-(hydroxymethyl)azetidin-1-yl)isoindoline-1,3-dione	90	112 mg
54	5-(3,6-dihydro-2H-pyran-4-yl)pyrazolo[1,5-a]pyrimidine	90	120 mg
55	N-(2,3-dihydro-1H-inden-4-yl)pivalamide	90	145 mg
56	N-(5-bromo-2,3-dihydro-1H-inden-4-yl)pivalamide	90	130 mg
57	1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidine-4-carbaldehyde	90	119 mg
58	piperidin-4-yl 4-methylbenzenesulfonate hydrochloride	90	126 mg
59	2-(2,6-dioxopiperidin-3-yl)-5-(4-((4-hydroxypiperidin-1-yl)methyl)piperidin-1-yl)isoindoline-1,3-dione	90	103 mg
60	2-(2,6-dioxopiperidin-3-yl)-5-fluoroisoindoline-1,3-dione	90	136 mg
61	(R)-4-(5-chloropyrazolo[1,5-a]pyrimidin-7-yl)-3-methylmorpholine	95	103 mg
62	methyl 3'-(methylsulfonyl)-[1,1'-biphenyl]-4-carboxylate	92	516 mg
63	1-(4-([1,1'-biphenyl]-4-yloxy)-2-bromophenyl)ethan-1-one	90	140 mg
64	3-(4-nitrophenoxy)aniline	99	588 mg
65	methyl 3-methyl-1H-indole-2-carboxylate	100	130 mg
66	methyl 6-(pyridin-4-yl)-1H-indole-2-carboxylate	95	310 mg
67	methyl 6-(benzyloxy)-1H-indole-2-carboxylate	91	120 mg
68	4-(3-nitrophenoxy)-1,1'-biphenyl	99	180 mg
69	methyl 7-bromo-4-fluoro-3-(2-methoxy-2-oxoethyl)-1H-indole-2-carboxylate	100	140 mg
70	3-(carboxymethyl)-6-phenethoxy-1H-indole-2-carboxylic acid	97	128 mg
71	methyl 2-amino-[1,1'-biphenyl]-4-carboxylate	96	235 mg
72	4-iodo-3-(trifluoromethyl)-1H-pyrazole	100	170 mg
73	(R)-4-(3,6-dichloropyridazin-4-yl)-3-methylmorpholine	98.28	200 mg
74	3,6-dichloro-N-((5-methylimidazo[1,2-a]pyridin-2-yl)methyl)pyridazin-4-amine	100	114 mg
75	ethyl 5-((tert-butoxycarbonyl)amino)pyrazolo[1,5-a]pyridine-3-carboxylate	98.84	150 mg
76	3-(2,6-difluoro-4-iodopyridin-3-yl)-N-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-3-yl)propanamide	98.77	185 mg
77	3-(6-chloro-5-(4,4-difluoropiperidin-1-yl)pyridazin-3-yl)-8-oxa-3-azabicyclo[3.2.1]octane	96.34	135 mg
78	(2S,6R)-4-(3,6-dichloropyridazin-4-yl)-2,6-dimethylmorpholine	99.53	670 mg
79	tert-butyl 4-(5-chloropyrazolo[1,5-a]pyrimidin-7-yl)-3,6-dihydropyridine-1(2H)-carboxylate	99.09	820 mg
80	3-(2,4-difluoro-6-iodophenyl)propanoic acid	92.14	1000 mg
81	8-bromo-2,4-dichloro-1,5-naphthyridine	95.72	270 mg
82	methyl 2-amino-4-bromo-3,5-difluorobenzoate	90	2.7 g
83	4-(4-aminophenoxy)benzenesulfonamide	90	755 mg
84	4-((4-chlorophenoxy)methyl)aniline	90	3.97 g
85	3'-amino-[1,1'-biphenyl]-3-sulfonamide	90	4.91 g
86	tert-butyl 4-(3-bromobenzoyl)piperazine-1-carboxylate	90	2.43 g
87	methyl 6-(benzyloxy)-3-(2-methoxy-2-oxoethyl)-1H-indole-2-carboxylate	90	135 mg
88	3-chloro-7-vinylisoquinoline	90	800 mg
89	2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione	90	330 mg
90	2-(2,6-dioxopiperidin-3-yl)-4-hydroxyisoindoline-1,3-dione	90	520 mg
91	([1,1'-biphenyl]-3-ylmethyl)triphenylphosphonium bromide	98.5	1.543 g
92	(4-phenoxybenzyl)triphenylphosphonium bromide	97.2	344 mg
93	1-(tert-butyl) 2-methyl 3-formyl-1H-indole-1,2-dicarboxylate	93.5	1.167 g
94	methyl 3-formyl-1H-indole-2-carboxylate	93.2	102 mg
95	2-(2,6-dioxopiperidin-3-yl)-5-methylisoindoline-1,3-dione	86.4	242 mg
96	((4'-(methoxycarbonyl)-[1,1'-biphenyl]-2-yl)methyl)triphenylphosphonium bromide	94.3	1.215 g
97	methyl 6-formyl-1H-indole-2-carboxylate	95.6	777 mg
98	methyl 3'-nitro-[1,1'-biphenyl]-2-carboxylate	96.5	243 mg
99	methyl (E)-3-(4-(([1,1'-biphenyl]-3-yloxy)methyl)phenyl)-2-azidoacrylate	83.6	221 mg
100	4-(benzyloxy)-2-nitrobenzenediazonium tetrafluoroborate	84.3	1.744 g
101	6-(benzyloxy)-3-(carboxymethyl)-1H-indole-2-carboxylic acid	98.7	230 mg
102	methyl 5-(pyridin-4-yl)-1H-indole-2-carboxylate	100	215 mg
103	methyl 4-amino-5-bromo-1,2-dihydropyridazine-3-carboxylate	99.157	230 mg
104	2-(methoxycarbonyl)-1H-indole-6-carboxylic acid	97.1	222 mg
105	2,4-dichloro-7-methoxy-1,8-naphthyridine	86.6	180 mg
106	3-methylthiomorpholine 1,1-dioxide hydrogen chloride	98.2	200 mg
107	3,3'-(3-iodopyrazolo[1,5-a]pyrimidine-5,7-diyl)bis(6-oxa-3-azabicyclo[3.1.1]heptane)	98.3	100 mg
108	4-([1,1'-biphenyl]-4-yloxy)benzaldehyde	98	160 mg
109	1-(tert-butyl) 2-methyl 6-bromo-1H-indole-1,2-dicarboxylate	100	180 mg
110	methyl 6-bromo-1H-indole-2-carboxylate	89	140 mg
111	methyl 6-([1,1'-biphenyl]-4-yloxy)-1H-indole-2-carboxylate	99	100 mg
112	4-([1,1'-biphenyl]-3-yloxy)benzaldehyde	100	450 mg
113	4-amino-3-nitrobenzaldehyde	98	120 mg
114	3-(carboxymethyl)-1H-indole-2-carboxylic acid	100	130 mg
115	3-(carboxymethyl)-1-isobutylindoline-2-carboxylic acid	100	130 mg
116	4-(3-nitrobenzyl)morpholine	100	250 mg
117	6-chloro-3-fluoro-5-vinylpyridin-2-amine	95	110 mg
118	3-(4-aminophenoxy)benzenesulfonamide	90	11.2 g
119	4-(difluoromethoxy)-3-isopropoxybenzoic acid	86.78	1.981 g
120	2-(3-methylisothiazol-5-yl)isoindoline-1,3-dione	91.94	2.232 g
121	N-((1H-1,2,4-triazol-3-yl)methyl)-2-ethoxybenzamide Molecular Weight: 246.27	87.14	1.025 g
122	3-(benzyloxy)-4-(difluoromethoxy)benzamide	88.43	456 mg
123	4-(3-(2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(2H-tetrazol-2-yl)propyl)bicyclo[1.1.1]pentan-1-yl)phenol	83.68	419 mg
124	methyl 5-cyanoquinoline-6-carboxylate	98.97	1.298 g
125	6-aminoquinoline-5-carbonitrile	98.09	2.017 g
126	2-ethoxy-N-(prop-2-yn-1-yl)benzamide	99.04	6.228 g
127	7a,9,10,11,12,12a-hexahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one	100	466 mg
128	(2-fluoro-6-methoxypyridin-3-yl)boronic acid	94.8	1080 mg
129	3-bromo-5-(naphthalen-1-yl)pyridine	96.3	1010 mg
130	ethyl 2-(7-methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-4-yl)oxazole-5-carboxylate	97.3	165 mg
131	4-bromo-2-ethoxyphenol	92.71	3470 mg
132	2-(7-methoxy-3H-spiro[benzofuran-2,1'-cyclopentan]-4-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane	97.28	12.182 g
133	2-(8-methoxy-2,2-dimethylchroman-5-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane	87.42	1.372 g
134	5-bromo-2-methoxyphenol	100	2.171 g
135	5-iodo-7-methoxy-3-methyl-3H-imidazo[4,5-b]pyridine	96	168 mg
136	2-bromo-6-fluoro-4-(trifluoromethyl)benzoic acid	100	1.9 g
137	tert-butyl (4-bromo-2,2,5-trifluoro-1-oxido-3-oxo-2,3-dihydro-1l4-benzo[b]thiophen-1-ylidene)carbamate	100	2.2 g
138	5-bromo-8-methoxy-2-(trifluoromethyl)quinoline	96.32	25.961 g
139	5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-amine	95	4.3 g
140	2-(5-amino-3-methyl-1H-pyrazol-1-yl)-6-propylpyrimidin-4(3H)-one	95	1.2 g
141	6-chloro-N-cyclohexyl-2-(pyridin-2-yl)pyrimidin-4-amine	95	4.1 g
142	N-(5-bromoquinolin-8-yl)-4-methylbenzenesulfonamide	90	640 mg
143	3-chloro-6-(methylthio)-N-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carboxamide	95	360 mg
144	3-chloro-N-(5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl)-N-methylbenzamide	95	70 mg
145	N-(3-methyl-1-(6-oxo-4-propyl-1,6-dihydropyrimidin-2-yl)-1H-pyrazol-5-yl)thiazole-2-carboxamide	95	188 mg
146	5-(2-methoxyphenyl)-N-(1-methyl-1H-benzo[d]imidazol-2-yl)-1,3,4-oxadiazol-2-amine	93	132 mg
147	N-(5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl)tetrahydro-2H-pyran-4-carboxamide	95	50 mg
148	N-(5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl)isobutyramide	94	134 mg
149	N-(5-bromoquinolin-8-yl)tetrahydro-2H-pyran-4-sulfonamide	95	72 mg
150	2-(pyridin-2-yl)pyrimidine-4,6-diol	90	4.1 g
151	5-bromo-6-nitroquinoline	90	1.3 g
152	6,7-dimethoxy-2-methylquinazolin-4-ol	100	11.3 g
153	7-(benzyloxy)-6-methoxy-2-methylquinazolin-4-ol	75	3.2 g
154	tert-butyl (S)-3-((7-methoxy-2-methyl-4-(((R)-1-(3-nitro-5-(trifluoromethyl)phenyl)ethyl)amino)quinazolin-6-yl)oxy)pyrrolidine-1-carboxylate	97	4.6 g
155	(S)-tetrahydrofuran-3-yl methanesulfonate	\	3.5 g
156	tert-butyl (R)-3-((methylsulfonyl)oxy)pyrrolidine-1-carboxylate	\	28.3 g
157	4-(benzyloxy)-5-hydroxy-2-nitrobenzoic acid	85	9.5 g
158	2-(3-azido-2-hydroxypropyl)isoindoline-1,3-dione	100	1.2 g
159	2-hydroxy-N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetamide	94	136 mg
160	4-(bis(4-methoxybenzyl)amino)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one	99	110 mg
161	4-amino-1-(3-fluoro-4-(pyrrolidin-1-ylmethyl)benzyl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one	98	105 mg
162	4-(2-(dimethylamino)ethoxy)benzonitrile	93	171 mg
163	2-(ethylthio)-1-(4-(pyrrolidin-1-ylmethyl)benzyl)-1H-imidazo[4,5-c]quinolin-4-amine	97	75 mg
164	tert-butyl 4-((5-cyanothiophen-2-yl)methyl)piperazine-1-carboxylate	99	105 mg
165	6-butoxy-1-(4-(pyrrolidin-1-ylmethyl)benzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine	100	110 mg
166	ethyl (Z)-4-((phenyldiazenyl)methyl)benzoate	93	135 mg
167	2-(chloromethyl)isoindoline-1,3-dione	90	4.5 g
168	2-(chloromethyl)isoindoline-1,3-dione	90	8.0 g
169	2-(chloromethyl)isoindoline-1,3-dione	90	6.9 g
170	2,2'-(pyridin-2-ylmethylene)diphenol	98	7.4 g
171	2,2'-(pyridin-2-ylmethylene)diphenol	98	1.5 g
172	benzyl(2-bromoethyl)sulfane	90	5.7 g
173	2-(chloromethyl)-1H-benzo[d]imidazole	90	4.28 g
174	5-fluoro-3-nitropicolinonitrile	95	9.7 g
175	5-bromo-3-(1,3-dioxolan-2-yl)-2-fluoropyridine	94	2.28 g
176	4-fluoroquinoline	94	2.9 g
177	2-cyclobutylacetonitrile	\	8.24 g
178	methyl (E)-4-bromo-3-((2-methyl-3-phenylallyl)oxy)benzoate	\	4.295 g
179	(Z)-N-((methylsulfonyl)oxy)acetimidoyl chloride	\	8.44 g
180	3-benzyl-3-methyl-2,3-dihydrobenzofuran-6-carboxylic acid	96	556 mg
181	2-((5-bromo-2-nitrophenyl)amino)-N-(2-hydroxyethyl)acetamide	95	110 mg
182	tert-butyl 4-(cyanomethylene)piperidine-1-carboxylate	95	100 mg
183	potassium (3,5-dimethylisoxazol-4-yl)trifluoroborate	95	19 g
184	methyl 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindoline-5-carboxylate	90	219.84 mg
185	ethyl (E)-3-(3,5-dichlorophenyl)acrylate	90	1986.44 mg
186	3-(1-oxo-5-vinylisoindolin-2-yl)piperidine-2,6-dione	90	831.19 mg
187	3-(4-methoxybenzyl)imidazolidine-2,4-dione	90	4484.23 mg
188	5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine	90	39.13 mg
189	2-oxo-2-(pyridin-3-yl)acetic acid	90	1428.28 mg
190	2,2,5-tribromo-2,3-dihydro-1H-inden-1-one	90	1622.07 mg
191	2,5-dibromo-2,3-dihydro-1H-inden-1-one	90	3929.72 mg
192	3-bromopiperidine-2,6-dione	90	321.23 mg
193	(E)-2-styrylthiophene	90	3319.16 mg
194	1-oxo-2,3-dihydro-1H-indene-5-carbonitrile	90	1328.26 mg
195	2-chloro-1-(3-hydroxyazetidin-1-yl)ethan-1-one	95	2.73 g
196	2-((2-cyclopropyl-8-fluoro-6-(4-(2-oxopropyl)piperazin-1-yl)quinolin-4-yl)(ethyl)amino)-4-(4-fluorophenyl)thiazole-5-carbonitrile	95	140 mg
197	2-((2-cyclopropyl-8-fluoro-6-(4-(2-hydroxypropyl)piperazin-1-yl)quinolin-4-yl)(ethyl)amino)-4-(4-fluorophenyl)thiazole-5-carbonitrile	97	75 mg
198	6-bromo-2-cyclopropyl-8-fluoro-N-methylquinolin-4-amine	97	566 mg
199	(9H-fluoren-9-yl)methyl (4-(chloromethyl)-2-methoxybenzyl)carbamate	93	410 mg
200	tert-butyl (R)-(3-(benzyloxy)-2-hydroxypropyl)(2,4-dimethoxybenzyl)carbamate	95	150 mg
201	tert-butyl (R)-(3-(benzyloxy)-2-hydroxypropyl)(2,4-dimethoxybenzyl)carbamate	95	4.28 g
202	N-((4-bromophenyl)sulfonyl)-3-methylbutanamide	95	12.0 g
203	methyl 5-(chloromethyl)-4'-(N-(3-methylbutanoyl)sulfamoyl)-[1,1'-biphenyl]-3-carboxylate	99	1.35 g
204	methyl 2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-oxo-4,5-dihydrothiophene-3-carboxylate	98	370 mg
205	methyl 4-(benzyloxy)-2,2-dimethylbutanoate	91	8.65 g
206	N-(3-(((2-chloro-5-iodopyrimidin-4-yl)amino)methyl)pyrazin-2-yl)-N-methylmethanesulfonamide	72	1.44 g
207	benzyl 3,3-difluorocyclobutane-1-carboxylate	80	17.4 g
208	1-chloro-7-methoxyisoquinoline-6-carbonitrile	95	1.36 g
209	methyl 3-bromo-5-(hydroxymethyl)benzoate	98	51.45 g
210	2-methoxybenzyl carbamimidothioate hydrochloride	95	22.13 g
211	tert-butyl 7-(methyl(7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-azaspiro[3.5]nonane-2-carboxylate	93	1000 mg
212	methyl 2-bromo-5H-pyrrolo[2,3-b]pyrazine-7-carboxylate	100	210 mg
213	2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)aniline	97	900 mg
214	2-methoxy-3-(1-methyl-1H-1,2,4-triazol-5-yl)aniline	95.7	500 mg
215	N-(3-methoxy-1,2,4-thiadiazol-5-yl)-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.5]nonane-1-carboxamide	99	700 mg
216	6-bromo-2-(2,6-dimethylpyridin-4-yl)-3-methyl-1H-indole	95	8.14 g
217	6-(3-isopropyl-5-(piperidin-4-yl)-1H-indol-2-yl)-7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridine hydrochloride	95	1.05 g
218	2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide	93	1.27 g
219	6-bromo-3-(piperidin-1-ylmethyl)-1H-pyrrolo[2,3-b]pyridine	96	648 mg
220	tert-butyl (2-((4-(1-(1-oxo-1,2-dihydroisoquinolin-5-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxamido)-6-(trifluoromethyl)pyridin-2-yl)oxy)ethyl)carbamate	95	295 mg
221	tert-butyl (1R,5S)-3-(7-bromo-6-chloro-8-fluoroquinazolin-4-yl)-3,8-diazabicyclo[3.2.1]octane-8-carboxylate	99	780 mg
222	methyl 2-(1,4-dioxaspiro[4.5]decan-8-yl)-5-(6-(trifluoromethyl)picolinamido)-2H-indazole-6-carboxylate	95	35 mg
223	N-(6-(2-hydroxypropan-2-yl)-2-(4-oxocyclohexyl)-2H-indazol-5-yl)-6-(trifluoromethyl)picolinamide	90	550 mg
224	tert-butyl 4-hydroxy-2-(methylthio)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate	\	6.85 g+8.05 g
225	tert-butyl (5-bromo-2-chloro-4-methylpyridin-3-yl)(tert-butoxycarbonyl)carbamate	\	8.23 g+5.10 g
226	2-((4-chloropyrimidin-5-yl)oxy)-5-fluoro-N,N-diisopropylbenzamide	\	9.62 g
227	tert-butyl (S)-10-bromo-11-chloro-8-(2-isopropylphenyl)-7-oxo-3,4,7,8,13,13a-hexahydropyrazino[2',1':3,4][1,4]oxazepino[5,6,7-de]quinazoline-2(1H)-carboxylate	\	1.47 g
228	tert-butyl (5-bromo-4-chloropyridin-3-yl)(tert-butoxycarbonyl)carbamate	\	5.93 g
229	7-fluoro-8-methylnaphthalen-1-yl trifluoromethanesulfonate	\	13.79 g
230	methyl 2-((4-chloropyrimidin-5-yl)oxy)-5-fluorobenzoate	\	2.87 g
231	7-bromo-5-fluoro-1-(2-isopropylphenyl)quinazoline-2,4(1H,3H)-dione	\	1.1 g
232	6-amino-4-bromo-3-chloro-2-fluorobenzonitrile	\	2.55 g
233	6-amino-4-bromo-3-chloro-2-fluorobenzonitrile	\	2.72 g
234	2-amino-4-bromo-6-fluorobenzonitrile	\	6.2 g
235	2-amino-4-bromo-6-fluorobenzonitrile	\	3 g
236	(R)-(1-((3-methylpyrrolidin-1-yl)methyl)cyclopropyl)methanol	\	0.72 g
237	(1-(morpholinomethyl)cyclopropyl)methanol	\	0.88 g
238	(1-(pyrrolidin-1-ylmethyl)cyclopropyl)methanol	\	9.83 g
239	(E)-1-(4-chloro-1-(1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-5-yl)-1H-benzo[d][1,2,3]triazol-6-yl)-3-(dimethylamino)prop-2-en-1-one	\	0.26 g
240	tert-butyl (tert-butoxycarbonyl)(4-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)carbamate	\	1 g
241	7-fluoro-8-methylnaphthalen-1-yl trifluoromethanesulfonate	\	1.7 g
242	methyl 2-((2S,6S)-6-methyl-4-((4-nitrophenyl)sulfonyl)piperazin-2-yl)acetate	\	17 g
243	1-benzyl 4-(tert-butyl) (S)-2-(cyanomethyl)piperazine-1,4-dicarboxylate	\	3.8 g
244	methyl 2-((2S,6S)-6-methyl-4-((4-nitrophenyl)sulfonyl)piperazin-2-yl)acetate	\	5.2 g
245	(S)-1-((benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid	\	180 mg
246	benzyl (S)-2-(cyanomethyl)piperazine-1-carboxylate	\	3.7 g
247	2-amino-4-bromo-6-fluorobenzonitrile	\	6.2 g
248	4-bromo-2,6-difluorobenzamide	\	5 g
249	2-amino-3-methyl-5-propylpyrazolo[1,5-a]pyrimidin-7(4H)-one	\	6.8 g
250	1-bromo-8-chloronaphthalene	\	5.18 g
251	8-benzyl-1,3,8-triazaspiro[4.5]decane-2,4-dione	\	1.7 g
252	4-bromo-2,6-difluoro-N-((2-isopropylphenyl)carbamoyl)benzamide	\	3.3 g
253	benzyl (2-chloro-9-isopropyl-9H-purin-6-yl)glycinate	\	0.86 g
254	tert-butyl 4-(3,3-dimethylpiperazin-1-yl)benzoate	\	37.7 g
255	4-(3,3-dimethylpiperazin-1-yl)benzoic acid	\	10 g
256	6-(2,6-dichloro-3,5-dimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amine	\	15 g
257	methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate	\	10 g
258	tert-butyl 4-(4-((benzyloxy)carbonyl)piperazin-1-yl)-2-(methylsulfonyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate	\	12 g
259	2-(4-fluorobenzyl)-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid	\	25 g
260	benzyl (4-bromo-2-cyanophenyl)carbamate	\	20 g
261	methyl 2-((2R,6R)-6-methyl-4-((4-nitrophenyl)sulfonyl)piperazin-2-yl)acetate	\	75 g
262	methyl 2-((2R,6R)-6-methyl-4-((4-nitrophenyl)sulfonyl)piperazin-2-yl)acetate	\	23 g
263	4-bromo-2,6-difluorobenzamide	\	21.6 g
264	tert-butyl (2-bromo-9-isopropyl-9H-purin-6-yl)glycinate	\	50.5 g
265	6-chloro-2-fluoro-9-isopropyl-9H-purine	\	31.6 g
266	tert-butyl (2-chloro-9-isopropyl-9H-purin-6-yl)glycinate	\	130 g
267	tert-butyl (2-bromo-9-isopropyl-9H-purin-6-yl)glycinate	\	164 g
268	methyl (E)-3-(2-([1,1'-biphenyl]-3-yl)vinyl)-6-bromo-1H-indole-2-carboxylate	90	116 mg
269	3-(carboxymethyl)benzofuran-2-carboxylic acid	90	1.2 g
270	2'-methyl-[1,1'-biphenyl]-3-amine	90	150 mg
271	methyl 3-(2-methoxy-2-oxoethyl)benzofuran-2-carboxylate	90	300 mg
272	4-(o-tolyl)pyridin-2-amine	90	150 mg
273	methyl (E)-6-bromo-3-(4-phenoxystyryl)-1H-indole-2-carboxylate	90	108 mg
274	3-vinyl-1,1'-biphenyl	90	155 mg
275	2-methyl-3'-vinyl-1,1'-biphenyl	90	190 mg
276	1-phenoxy-2-vinylbenzene		101 mg
277	4-(([1,1'-biphenyl]-2-yloxy)methyl)-2-bromobenzoic acid	95	120 mg
278	methyl 3-(2-hydroxyethyl)-1H-indole-2-carboxylate	100	130 mg
279	methyl 2'-amino-[1,1'-biphenyl]-4-carboxylate	95	130 mg
280	3-(carboxymethyl)-1-ethyl-1H-indole-2-carboxylic acid	100	100 mg
281	2-nitro-5-phenoxypyridine	99	130 mg
282	1-(2-bromo-4-((2'-methyl-[1,1'-biphenyl]-3-yl)oxy)phenyl)ethan-1-one	95	100 mg
283	methyl 6-benzyl-1H-indole-2-carboxylate	96	100 mg
284	2-(methoxycarbonyl)-1H-indole-6-carboxylic acid	90	121 mg
285	2-phenoxybenzaldehyde	100	221mg
286	methyl 2-(2-([1,1'-biphenyl]-3-ylamino)-2-oxoethyl)-4-aminobenzoate	90	125 mg
287	methyl 6-hydroxy-3-(2-methoxy-2-oxoethyl)-1H-indole-2-carboxylate	90	140 mg
288	tert-butyl (6-(4-(hydroxymethyl)phenoxy)hexyl)carbamate	90	164 mg
289	tert-butyl (4-(4-(hydroxymethyl)phenoxy)butyl)carbamate	90	329 mg
290	6-((4-((8-aminooctyl)oxy)benzyl)oxy)-3-(4-phenoxyphenethyl)-1H-indole-2-carboxylic acid	90	45 mg
291	6-((4-((8-aminooctyl)oxy)benzyl)oxy)-3-(2-oxo-2-((4-phenoxyphenyl)amino)ethyl)-1H-indole-2-carboxylic acid	90	127 mg
292	5-methyl-2-nitrobenzenediazonium	90	500 mg
293	4'-nitro-[1,1'-biphenyl]-4-ol	94.5	593 mg
294	MC21-1687-033	90	111 mg
295	MC-4034-118	90	122 mg
296	MC211417-126	90	110 mg
297	MC21-1702-023	90	106mg
298	MC21-1702-027	90	110mg
299	MC21-1686-048	90	137mg
300	MC21-1686-033	90	106mg
301	MC21-1659-012	90	105mg
302	MC21-1659-040	90	103mg
303	((benzyloxy)carbonyl)glycine	100	3 g
304	2-chloro-3-nitro-N-(4-(pyrrolidin-1-ylmethyl)benzyl)quinolin-4-amine	92.7	1 g
305	1-(4-aminobutyl)-2-(methylthio)-1H-imidazo[4,5-c]quinolin-4-amine	99	200 mg
306	ethyl glycinate	98	1.5 g
307	2-(methylthio)-1-((5-(pyrrolidin-1-ylmethyl)quinolin-8-yl)methyl)-1H-imidazo[4,5-c]quinolin-4-amine	98.3	89 mg
308	5-methylquinoline-8-carbonitrile	100	383 mg
309	2-butoxy-6-chloro-N,N-bis(4-methoxybenzyl)-5-nitropyrimidin-4-amine	100	337 mg
310	8-bromo-5-methylquinoline	96.2	314 mg
311	2-(butylthio)-6-chloro-N4,N4-bis(4-methoxybenzyl)pyrimidine-4,5-diamine	94.3	209 mg
312	(2-amino-4-(methoxycarbonyl)phenyl)boronic acid	98.8	157 mg
313	N-(4-(4-amino-2-(methylthio)-1H-imidazo[4,5-c]quinolin-1-yl)butyl)-4-((2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl)cyclohexane-1-carboxamide	91.6	55mg
314	methyl 4-carbamoyl-2-nitrobenzoate	99	185 mg
315	tert-butyl 1-(9H-fluoren-9-yl)-3,7-dioxo-2,11,14-trioxa-4,8-diazaheptadecan-17-oate	98.7	210mg
316	3-nitroquinoline-2,4-diol	99.6	250mg
317	(6-(4-methylpiperazin-1-yl)pyridin-3-yl)methanamine	99.6	200mg
318	tert-butyl 4-(methoxy(methyl)carbamoyl)piperidine-1-carboxylate	88	141 mg
319	methyl 4-(([1,1'-biphenyl]-3-yloxy)methyl)-2-bromobenzoate	98	350 mg
320	4-(([1,1'-biphenyl]-3-yloxy)methyl)-2-bromo-N-methoxy-N-methylbenzamide	100	300 mg
321	3-(carboxymethyl)-6-(trifluoromethyl)-1H-indole-2-carboxylic acid	94	50 mg
322	6-benzyl-3-(1-carboxyethyl)-1H-indole-2-carboxylic acid	95	60 mg
323	9H-benzo[4,5]imidazo[2,1-c][1,2,4]triazol-3-amine	93	213mg
324	1-(2,4-bis(methoxymethoxy)phenyl)ethan-1-one	95	221 mg
325	(S)-2-((naphthalen-1-yloxy)methyl)oxirane	97	221 mg
326	(R)-2-((naphthalen-1-yloxy)methyl)oxirane	77	206 mg
327	2-allyl-4-nitrophenol	99	210 mg
328	pyrido[2,3-d]pyridazin-8(7H)-one	85	202 mg
329	2-chloro-1H-benzo[d]imidazole-1-carbonitrile	99	221 mg
330	3-(benzylamino)-1,1,1-trifluoropropan-2-ol	\	7.2 g
331	methyl N-(tert-butoxycarbonyl)-O-(tert-butyldiphenylsilyl)-D-serinate	\	8.9 g
332	methyl O-benzyl-N-(tert-butoxycarbonyl)-D-serinate	\	3.6 g
333	2-chloro-5,6,7,8-tetrahydro-1,6-naphthyridine	\	6.5 g
334	(tert-butoxycarbonyl)-L-proline	\	8 g
335	tert-butyl piperidin-4-ylcarbamate	\	4.8 g
336	4-(2-fluoropyridin-3-yl)-2-(methylthio)pyrimidine	100	110 mg
337	2-methoxy-5-methyl-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)aniline	100	200 mg
338	tert-butyl (S)-4-(2-hydroxyquinoxalin-6-yl)-2-methylpiperazine-1-carboxylate	91	115 mg
339	4-methylbenzyl carbamimidothioate	93	120 mg
340	5-bromo-7-methoxy-2-methyl-2H-indazole	100	105 mg
341	2,7-dimethylpyrazolo[1,5-a]pyridine-5-carbonitrile	100	103 mg
342	(S)-6-(3-methylpiperazin-1-yl)benzo[d]thiazole	98	110 mg
343	5-bromo-7-methoxy-1-methyl-1H-indazole	99	102 mg
344	6-bromo-2-methylimidazo[1,2-a]pyrazine	95	150 mg
345	tert-butyl (S)-4-(benzo[d]thiazol-6-yl)-2-methylpiperazine-1-carboxylate	90	202 mg
346	5-bromopyrazin-2-amine	98	150 mg
347	tert-butyl (S)-4-(6-aminopyridazin-3-yl)-2-methylpiperazine-1-carboxylate	99	100 mg
348	7-methoxy-3-nitroquinolin-4-ol	94	105mg
349	2-bromo-6-chloro-4-methylpyridin-3-amine	98	100 mg
350	ethyl 4-chloro-6-fluoro-7-methoxyquinoline-3-carboxylate	98	110 mg
351	N-(4-bromo-2,6-difluorobenzyl)-7-methoxy-3-nitroquinolin-4-amine	100	110 mg
352	6-chloro-2,8-dimethylimidazo[1,2-b]pyridazine	99	113 mg
353	tert-butyl (4-methoxypyridin-2-yl)carbamate	97	100 mg
354	5-bromo-7-methoxy-2-methyl-2H-pyrazolo[3,4-c]pyridine	99	116 mg
355	4-chloro-7-methoxy-3-nitroquinoline	98	150 mg
356	N2-(4-chlorophenyl)-N6-cyclopropyl-3-nitropyridine-2,6-diamine	100	3.0g
357	3-(4-(benzyloxy)phenyl)-4-iodo-1H-pyrazole	100	3.1g
358	ethyl 5-morpholinopyrazolo[1,5-a]pyrimidine-3-carboxylate	91	2.9g
359	6-chloro-2-iodo-N-(4-methoxybenzyl)pyrimidin-4-amine	91.27	4.8g
360	2-methoxy-4-methylbenzoic acid	100	3.1g
361	benzyl 4-(tosyloxy)piperidine-1-carboxylate	100	4.4g
362	5-morpholinopyrazolo[1,5-a]pyrimidine-3-carboxylic acid	100	0.9g
363	3-aminopicolinonitrile	100	1.3g
364	5-bromo-2-methoxy-3-nitrobenzamide	74.48	2.1g
365	ethyl 5-(2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)pyrazolo[1,5-a]pyrimidine-3-carboxylate	100	1.3g
366	2-(5,6-dichloropyridin-3-yl)acetonitrile	83.61	2.1g
367	2-hydroxy-3-nitrobenzamide	98.9	8.1g
368	4-iodo-3-(4-phenoxyphenyl)-1H-pyrazole	76.69	4.3g
369	5-bromopicolinamide	100	4.6g
370	2-chloro-5-nitropyridin-4-amine	100	4.5g
371	3-aminopicolinamide	97.42	4.9g
372	5-nitroisothiazole-3-carboxylic acid	100	5.2g
373	tert-butyl 3-(2,5-dioxo-4-(pyridin-2-yl)imidazolidin-4-yl)propanoate	100	0.9g
374	7-chloro-1,3,4,5-tetrahydro-2H-benzo[d]azepin-2-one	100	2.6g
375	methyl 6-chloro-4-((3-((2,2,2-trifluoroacetamido)methyl)phenyl)thio)pyridazine-3-carboxylate	100	0.3g
376	3-aminopicolinamide	100	1.0g
377	N-(5-bromo-8-(methylamino)-4a,8a-dihydropyrido[3,4-c]pyridazin-3-yl)cyclopropanecarboxamide	100	0.2g
378	ethyl 5-amino-1-(4-methoxybenzyl)-1H-pyrazole-4-carboxylate	100	0.8g
379	4-bromo-2-ethoxy-6-nitroaniline	100	2.9g
380	tert-butyl (5-(4-aminopyrimidin-2-yl)thiazol-2-yl)(pent-4-en-1-yl)carbamate	100	2.0g
381	N4-(1-methylpiperidin-4-yl)-5-(trifluoromethyl)benzene-1,2,4-triamine	94	0.9g
382	5-bromo-2-hydroxy-4-methoxynicotinonitrile	84	0.2g
383	1H-indol-4-amine	97.76	5.1g
384	tert-butyl (1-(pyrimidin-2-yl)butyl)carbamate	100	3.0g
385	1-(4-amino-5-nitropyridin-2-yl)piperidin-4-ol	100	0.6g
386	tert-butyl (5-(4-aminopyridin-2-yl)thiazol-2-yl)(pent-4-en-1-yl)carbamate	94	0.6g
387	5-(hydroxymethyl)-2-methylphenol	100	1.7g
388	1-(2-chloro-5H-pyrrolo[2,3-d]pyrimidin-5-yl)propan-1-one	100	0.9g
389	tert-butyl (5-(4-aminopyrimidin-2-yl)thiazol-2-yl)(pent-4-en-1-yl)carbamate	100	2.1g
390	methyl 2-acrylamido-4-((tert-butoxycarbonyl)(2-(tosyloxy)propyl)amino)benzoate	100	0.6g
391	N-(1-(4-bromobenzoyl)piperidin-4-yl)acetamide	100	0.6g
392	4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridin-2(1H)-one	100	2.5g
393	4-chloro-3-(6-(2-methyl-6-methylenemorpholino)-1H-imidazo[4,5-c]pyridin-2-yl)-3,4-dihydroquinolin-2(1H)-one	40	1.2g
394	2-methoxy-1-(pyrimidin-2-yl)ethan-1-amine	100	1.3g
395	tert-butyl (2-methyl-1-(pyrimidin-2-yl)propyl)carbamate	100	1.0g
396	cyclohexyl(pyrimidin-2-yl)methanamine	85	3g
397	2,6-difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol	85	1.2g
398	8-(aminomethyl)-3-benzyl-2-hydroxy-4H-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one	100	0.1g
399	N-(3-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)ureido)pyrimidin-4-yl)amino)-1-methyl-2,3-dihydro-1H-pyrazol-4-yl)acrylamide	100	0.5g
400	2-Aminothiazole	100	1.4g
401	4-(4-cyclohexylpiperazin-1-yl)benzene-1,2-diamine	75	1.1g
402	4-(4-bromo-3-methoxyphenyl)-1-methyl-1H-pyrazole	100	5.0g
403	1-(3-bromopyridin-2-yl)piperidine-4-carbohydrazide	100	1.4g
404	(4-bromophenyl)(3-(hydroxymethyl)cyclopentyl)methanone	100	1.6g
405	3-(3-bromo-2-methoxyphenyl)-1-methyl-1H-1,2,4-triazole	100	5.5g
406	7-bromo-3-methylene-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine	100	1.5g
407	(4-chloro-3-nitrophenyl)dimethylphosphine oxide	100	4.3g
408	4-bromo-9H-pyrido[3,4-b]indole	84	4.4g
409	2-((3-amino-4-nitrophenyl)amino)ethan-1-ol	100	3.9g
410	tert-butyl (1-(3-methylpyridin-2-yl)ethyl)carbamate	100	0.8g
411	2-nitro-5-(2,2,6-trimethylmorpholino)aniline	100	4.2g
412	1-(4-amino-5-nitropyridin-2-yl)azetidin-3-ol	100	0.8g
413	5-(3-bromo-2-methoxyphenyl)-4,5-dihydrooxazole	100	3.7g
414	2-methoxy-5-nitropyridin-4-amine	100	2.9g
415	5-(4-chloro-2-fluoro-5-methoxyphenyl)-1-(difluoromethyl)-2-methyl-1,2-dihydro-3H-pyrazol-3-one	100	2.7g
416	2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenol	100	1.5g
417	N-(4-(1-methoxyvinyl)phenyl)acrylamide	100	1.2g
418	8-(trifluoromethyl)quinazolin-4-ol	59	4.7g
419	ethyl 4-bromothiazole-5-carboxylate	98	3.9g
420	2-methoxy-4-morpholinobenzoic acid	100	108g
421	2-carbamoyl-1-(4-chloro-2-methylphenyl)-6-methoxy-1,2,3,4-tetrahydroisoquinolin-7-yl trifluoromethanesulfonate	100	8.1g
422	3-(trifluoromethyl)benzohydrazide	100	8.9g
423	N-(4-bromobenzyl)-2,2,2-trifluoroacetamide	100	10.9g
424	methyl 6-chloro-4-((2-(methylthio)phenyl)amino)nicotinate	100	2.6g
425	4-iodo-2-methoxynicotinaldehyde	78	9.2g
426	2-bromo-3,4-dichloro-5-methyl-6-nitroaniline	100	7.3g
427	4-fluoro-5-morpholinobenzene-1,2-diamine	100	8g
428	7-chloro-4-(4-methoxybenzyl)-2-methyl-5-oxo-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-b]pyridine-6-carbaldehyde	93.4	102.1g+37.5g
429	5-bromo-2-methoxy-3-nitrobenzamide	88.5	15.42g
430	4-(benzyloxy)-2-naphthoic acid	92.79	115.1g+52.4g
431	4-bromophenol	100	41.4g
432	7-chloro-2-ethyl-4-(4-methoxybenzyl)-5-oxo-4,5-dihydro-2H-[1,2,3]triazolo[4,5-b]pyridine-6-carbaldehyde	78	161.1g+88.9g
433	methyl 6-chloro-4-((2-(methylthio)phenyl)amino)nicotinate	100	3.9g
434	tert-butyl 3-carbamoylazetidine-1-carboxylate	100	7.6g
435	N-(3-bromobenzyl)-2,2,2-trifluoroacetamide	100	7.5g
436	5-bromothiazol-2-amine	100	43.8g
437	5-bromo-4-iodo-2-methoxynicotinaldehyde	91	6.3g
438	1-(2-chloro-7-(pent-4-en-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)propan-1-one	100	15.1g
439	4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-	99	4.4g
440	7-nitro-1-tosyl-1H-indole	95	8.5g
441	methyl 5-methyl-1H-pyrazole-3-carboxylate	100	142.5g
442	2-(4-hydroxy-3-nitrophenyl)acetic acid	100	27.2g
443	7-chloro-2-ethyl-4-(4-methoxybenzyl)-5-oxo-4,5-dihydro-2H-pyrazolo[4,3-b]pyridine-6-carbaldehyde	100	3.4g
444	6-chloro-4-methylpyridazin-3(2H)-one	100	3.6g
445	N-(3-chloro-4-methoxy-2-nitrophenyl)acetamide	100	3g
446	2-fluoro-3-morpholino-6-nitroaniline	80.7	10.7g
447	ethyl 5-morpholinopyrazolo[1,5-a]pyrimidine-3-carboxylate	100	7.4g
448	4-nitro-1H-indole	93	45.3g
449	5-(1-methoxyvinyl)-4-nitro-1H-pyrazole	100	28g
450	tert-butyl (2-methyl-1-(pyridin-2-yl)propyl)carbamate	100	16.9g
451	5-([1,4'-bipiperidin]-1'-yl)-2-nitroaniline	100	7.9g
452	tert-butyl (E)-3-(4-morpholinophenyl)acrylate	99	1753mg
453	2-(5-fluoro-1H-indol-3-yl)-2-oxoacetic acid	99	982mg
454	2-(7-chloro-1H-indol-3-yl)-2-oxoacetic acid	99	484mg
455	2-(7-fluoro-1H-indol-3-yl)-2-oxoacetic acid	99	1006mg
456	2-(5-methoxy-1H-indol-3-yl)-2-oxoacetic acid	99	2001mg
457	tert-butyl (E)-3-(4-(4-methylpiperazin-1-yl)phenyl)acrylate	99	2187mg
458	2-(5-methyl-1H-indol-3-yl)-2-oxoacetic acid	99	807mg
459	2-(7-methyl-1H-indol-3-yl)-2-oxoacetic acid	99	2089mg
460	2-(6-methoxy-1H-indol-3-yl)-2-oxoacetic acid	99	1877mg
461	2-(6-methyl-1H-indol-3-yl)-2-oxoacetic acid	99	924mg
462	2-(5-chloro-1H-indol-3-yl)-2-oxoacetic acid	99	297mg
463	4-(piperidin-1-yl)benzaldehyde	99	1657mg
464	4-morpholinobenzaldehyde	99	1786mg
465	2-(4-methoxy-1H-indol-3-yl)-2-oxoacetic acid	99	2231mg
466	2-(4-chloro-1H-indol-3-yl)-2-oxoacetic acid	99	1729mg
467	5-phenyl-3,4-dihydronaphthalen-1(2H)-one	99	103 mg
468	methyl 6-(benzyloxy)-1H-indole-2-carboxylate	95	121 mg
469	methyl 3-(4-(cyclohexyloxy)phenethyl)-6-methoxy-1H-indole-2-carboxylate	95	100 mg
470	1-allyl-3-(cyclohexyloxy)benzene	90	115 mg
471	methyl 6-phenoxy-1H-indole-2-carboxylate	90	125 mg
472	methyl 6-(3-((tert-butyldimethylsilyl)oxy)propyl)-1H-indole-2-carboxylate	95	130 mg
473	3-vinyl-1,1'-biphenyl	99	105 mg
474	2-(2,6-difluoro-4-(methylthio)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane	90	480 mg
475	(3,5-difluorophenyl)(methyl)sulfane	90	220 mg
476	3-(2-bromo-3-methylphenyl)propan-1-ol	90	350 mg
477	3'-bromo-2-methyl-1,1'-biphenyl	90	587 mg
478	methyl 3-(2-hydroxyethyl)-6-methyl-1H-indole-2-carboxylate	90	113 mg
479	1-(benzyloxy)-4-(4-vinylphenoxy)benzene	90	133 mg
480	1-(4-vinylphenyl)piperidine		125 mg
481	phenyl(2-vinylphenyl)methanone	95	265 mg
482	3-(2-(2'-methyl-[1,1'-biphenyl]-3-yl)ethyl)-1H-indole-2-carboxylic acid	98	50 mg
483	3-(3-fluorophenyl)-1-vinylbenzene	90	131 mg
484	2-chloro-1-(3-vinylphenyl)benzene	90	153 mg
485	4-fluoro-1-(3-vinylphenyl)benzene	90	204 mg
486	4-(phenyloxy)-1-(prop-2-enyl)benzene	90	134 mg
487	4-{[3-(benzyloxy)phenyl]oxy}benzene-1-carbaldehyde	90	143 mg
488	phenyl(4-vinylphenyl)methanone	90	118mg
489	methyl 3-[(1E)-2-[3-(3-fluorophenyl)phenyl]vinyl]-1H-indole-2-carboxylate	90	104mg
490	methyl 3-[(1E)-2-[3-(2-chlorophenyl)phenyl]vinyl]-1H-indole-2-carboxylate	90	106mg
491	methyl 3-[(1E)-2-(4-{[3-(benzyloxy)phenyl]oxy}phenyl)vinyl]-1H-indole-2-carboxylate	90	105mg
492	3-[3-methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]propan-1-ol	90	105mg
493	3-(4-bromo-3-methylphenyl)prop-2-yn-1-ol	90	120mg
494	3'-methoxy-2,3,4,5-tetrahydro-1,1'-biphenyl	90	101 mg
495	3-cyclohexylphenol	98	156 mg
496	4-((3-cyclohexylphenoxy)methyl)benzaldehyde	90	182 mg
497	3-cyclohexylaniline	93	156mg
498	ethyl 2-(4-acetylphenyl)acetate	98	186 mg
499	4-(4-cyclohexylphenoxy)benzaldehyde	96	203 mg
500	4-(4-fluorophenoxy)benzaldehyde	99	197 mg
501	methyl (E)-6-(3-((tert-butyldimethylsilyl)oxy)propyl)-3-(2-(2'-methyl-[1,1'-biphenyl]-3-yl)vinyl)-1H-indole-2-carboxylate	95	169 mg
502	2-bromo-5-phenyl-1,2,3,4-tetrahydronaphthalen-1-ol	97	143 mg
503	methyl (E)-3-(3-bromostyryl)-1H-indole-2-carboxylate	99	102 mg
504	methyl (E)-2-azido-3-(4-((3-cyclohexylphenoxy)methyl)phenyl)acrylate	96	118 mg
505	2-methyl-1-nitro-4-phenoxybenzene	96	243 mg
506	methyl 3-(2-(2'-methyl-4-(3-((methylsulfonyl)oxy)propyl)-[1,1'-biphenyl]-3-yl)ethyl)-1H-indole-2-carboxylate	90	56 mg
507	(R)-4-benzyl-3-((S)-2-(3-chloropropyl)pent-4-enoyl)oxazolidin-2-one	90	135 mg
508	(S)-2-(3-chloropropyl)pent-4-en-1-ol	90	110 mg
509	5-allyl-1,3-dioxane	90	120 mg
510	(S)-2-(tetrahydro-2H-pyran-3-yl)acetic acid	90	65 mg
511	methyl 3-(2-(6-(3-hydroxypropyl)-2'-methyl-[1,1'-biphenyl]-3-yl)ethyl)-1H-indole-2-carboxylate	95	100mg
512	methyl 6-bromo-3-(2-ethoxy-2-oxoethyl)-1H-indole-2-carboxylate	100	110mg
513	3'-ethynyl-4-fluoro-2-methyl-1,1'-biphenyl	95	120mg
514	tert-butyl (4-(4-formylphenoxy)butyl)carbamate	100	110mg
515	methyl 6-(3-(3-hydroxypropyl)phenoxy)-1H-indole-2-carboxylate	98	140mg
516	3-(3-hydroxypropyl)phenol	95	120mg
517	4-(4-phenoxyphenoxy)benzaldehyde	96	110mg
518	methyl 6-methyl-1H-indole-2-carboxylate	98	100mg
519	methyl 6-([1,1'-biphenyl]-3-yloxy)-1H-indole-2-carboxylate	100	150mg
520	4-(3-(3-hydroxypropyl)phenoxy)benzaldehyde	94	150mg
521	4-((2'-methyl-[1,1'-biphenyl]-4-yl)oxy)benzaldehyde	100	150mg
522	5-bromo-N-(3-nitrophenyl)pentanamide	95	120mg
523	1-(3-nitrophenyl)piperidin-2-one	100	100mg
524	methyl 6-(4-phenoxyphenoxy)-1H-indole-2-carboxylate	100	100mg
525	3-(carboxymethyl)-7-methyl-1H-indole-2-carboxylic acid	95	100mg
526	1-(3-aminophenyl)piperidin-2-one	95	200mg
527	2-([1,1'-biphenyl]-4-yloxy)-4-fluorobenzaldehyde	95	100mg
528	N-(5-bromo-2,3-dihydro-1H-inden-4-yl)pivalamide	100	100 mg
529	3-(6-chloro-5-((R)-3-methylmorpholino)pyridazin-3-yl)-8-oxa-3-azabicyclo[3.2.1]octane	95	230 mg
530	3-(6-chloro-5-(3,3-dimethylmorpholino)pyridazin-3-yl)-8-oxa-3-azabicyclo[3.2.1]octane	96	220 mg
531	5-(2-fluoropyridin-4-yl)-2,3-dihydro-1H-inden-4-amine	85	372 mg
532	(R)-4-(7-iodopyrazolo[1,5-a]pyrimidin-5-yl)-3-methylmorpholine	93	100 mg
533	4-bromo-3,6-dichloropyridazine	99	515 mg
534	3,6-dichloro-4-(piperidin-1-yl)pyridazine	98	204 mg
535	3-ethyl 5-methyl 6-bromoimidazo[1,2-a]pyridine-3,5-dicarboxylate	91	151 mg
536	(1R,5S)-3-(pyrazolo[1,5-a]pyrimidin-5-yl)-8-oxa-3-azabicyclo[3.2.1]octane	96	136 mg
537	3-ethyl 5-methyl 8-bromoimidazo[1,2-a]pyridine-3,5-dicarboxylate	95	313 mg
538	N-(2,3-dihydro-1H-inden-4-yl)pivalamide	100	100 mg