Table 1.

ATR/CHK1 inhibitors discussed in this review.

Agents	Targets	Preclinical research	Treatment	Clinical trials	Detail	References
UCN-01	CHK1	cellular/xenograft	Cisplatin	NCT00045513	Phase I/II combined with fludarabine phosphate	[40–44,62,136– 138,146,203,217]
	CHK2		Doxorubicin	NCT00006464	Phase I combined with cisplatin
	CDK1		HDAC inhibitor	NCT00004059	Phase I combined with fluorouracil
	CDK2			NCT00030888	Phase II single
	MK2			NCT00072267	Phase II combined with topotecan hydrochloride
	PKC			NCT00019838	Phase I combined with fludarabine phosphate
				NCT00003289	Phase I single
				NCT00042861	Phase I combined with multiple chemo drugs
				NCT00047242	Phase I combined with irinotecan hydrochloride
				NCT00045500	Phase I combined with prednisone
				NCT00045747	Phase II combined with fluorouracil
				NCT00045175	Phase I combined with topotecan hydrochloride
				NCT00001444	Phase I single
				NCT00072189	Phase II single
				NCT00012194	Phase I combined with cisplatin
				NCT00301938	Phase I combined with perifosine
				NCT00098956	Phase II combined with topotecan hydrochloride
				NCT00031681	Phase I combined with irinotecan hydrochloride
				NCT00039403	Phase I combined with gemcitabine
				NCT00004263	Phase I combined with cytarabine
				NCT00082017	Phase II single
				NCT00036777	Phase I combined with carboplatin
XL844	CHK1	cellular/xenograft	Gemcitabine	NCT00475917	Phase I single/combined with gemcitabine	[45]
	CHK2			NCT00234481	Phase I single
	VEGFR-2
	VEGFR-3
CBP501	CHK1	cellular/xenograft	CDDP	NCT00700336	Phase I/II combined with pemetrexed and cisplatin	[46–48]
	CHK2		Bleomycin	NCT00551512	Phase I combined with cisplatin
	MAPKAP-K2		Cisplatin	NCT00942825	Phase II combined with cisplatin and pemetrexed
	c-Tak1		Pemetrexed
	PLK1
AZD7762	CHK1	Cellular/xenograft	Nocodazole	NCT00937664	Phase I single/combined with gemcitabine	[49–59,65– 68,139,196,210,211]
	CHK2		Camptothecin	NCT00413686	Phase I single/combined with gemcitabine
			Gemcitabine	NCT00473616	Phase I single/combined with irinotecan
			Irinotecan
			Gemcitabine
			Radiation
			Cisplatin
			Temozolomide
			HDAC inhibitor
LY2603618	CHK1	Cellular/xenograft	Gemcitabine	NCT00415636	Phase I combined with pemetrexed	[69–74]
			Pemetrexed	NCT00839332	Phase I/II combined with gemcitabine
			Cisplatin	NCT00988858	Phase II combined with pemetrexed
				NCT01296568	Phase I single
				NCT01139775	Phase I/II combined with gemcitabine or pemetrexed
				NCT01341457	Phase I combined with gemcitabine
				NCT01358968	Phase I single
MK-8776	CHK1	Cellular/xenograft	Antimetabolites	NCT01870596	Phase II combined with cytarabine	[75–83,135,140,189,196]
			Gemcitabine	NCT00779584	Phase I/II combined with gemcitabine
			Radiation	NCT00907517	Phase I combined with cytarabine
			Pemetrexed	NCT01521299	Phase I combined with hydroxyurea
			Cytarabine
PF-00477736	CHK1	Cellular/xenograft	Gemcitabine	NCT00437203	Phase I combined with gemcitabine	[84–88,153,188]
			Carboplatin
			Docetaxel
			Radioimmunotherapy
			Radiation
LY2606368	CHK1	Cellular/xenograft	BMN673	NCT01115790	Phase I single	[89,90]
	CHK2			NCT02873975	Phase II single
				NCT02203513	Phase II single
				NCT02808650	Phase I single
				NCT02514603	Phase I single
				NCT02860780	Phase I combined with ralimetinib
				NCT02555644	Phase I combined with radiation and multiple chemo drugs
				NCT02735980	Phase II single
				NCT02124148	Phase I combined with multiple chemo drugs
				NCT02778126	Phase I single
				NCT02649764	Phase I combined with fludarabine and cytarabine
2e	CHK1	Cellular/xenograft	Doxorubicin			[91]
			Camptothecin
CCT244747	CHK1	Cellular	Radiation			[92–94]
			Gemcitabine
CHIR-124	CHK1	Cellular/xenograft	Radiation			[95–97]
			Top1 inhibitor
			HDAC inhibitor
GNE-783	CHK1	Cellular	Temozolomide			[98]
GNE-900	CHK1	Cellular/xenograft	Gemcitabine			[98]
			CPT-11
			Temozolomide
PD-321852	CHK1	Cellular	Gemcitabine			[99]
	Wee1
PD-407824	CHK1	Cellular	Gemcitabine			[100]
	Wee1
SAR-020106	CHK1	Cellular/xenograft	Radiation			[101–104]
			Radiochemo
SB-218078	CHK1	Cellular	Doxorubicin			[62,105–107]
			HSP inhibitor
S1181	CHK1	Cellular	Gemcitabine			[108]
V158411	CHK1	Cellular/xenograft	Irinotecan			[109]
	CHK2
CH-1	CHK1 Aurora A	Cellular	Hypoxia			[181]
AR323	CHK1	Cellular				[154]
AR678	CHK1	Cellular				[154]
AR458323	CHK1	Cellular	MK-1775			[187]
Schisandrin B	ATR	Cellular	UV			[110,111]
NU6027	CDK2	Cellular	PARP inhibitor			[112,113,205]
	CDK1		Hydroxyurea
	DNA-PK		Cisplatin
	ATR
NVP-BEZ235	PI3K	Cellular				[114]
	MTOR
	ATR
	ATM
	DNA-PKcs
Torin 2	MTOR	Cellular				[115]
	ATR
	ATM
	DNA-PKcs
ETP-46464	MTOR	Cellular				[114]
	ATR
	ATM
	DNA-PKcs
	PI3K
Compound	ATR	Cellular	Cisplatin			[116]
45
VE-821	ATR	Cellular/xenograft	Radiation			[53,117– 125,158,192,199,205]
			Cisplatin
			Topotecan
			Veliparib
VE-822 (VX-970)	ATR	Cellular/xenograft	Radiation	NCT02157792	Phase I combined with multiple chemo drugs	[124,126–128]
			Cisplatin	NCT02627443	Phase II combined with multiple chemo drugs
				NCT02567409	Phase II combined with multiple chemo drugs
				NCT02487095	Phase I/II combined with Topotecan
				NCT02595892	Phase II combined with Gemcitabine
				NCT02589522	Phase I combined with radiotherapy
				NCT02567422	Phase I combined with Cisplatin
				NCT02595931	Phase I combined with Irinotecan
				NCT02723864	Phase I combined with Veliparib and Cisplatin
AZ20	ATR	Cellular				[129]
AZD6738	ATR	Cellular/xenograft	Radiation	NCT02264678	Phase I/Ib combined with multiple chemo drugs	[130–133]
			Cisplatin	NCT02223923	Phase I single/combined with radiotherapy
			Top1 inhibitor	NCT01955668	Phase I single
				NCT02630199	Phase I combined with Paclitaxel

Clinical trial data are from https://clinicaltrials.gov/.