Table 1.

SERCA inhibitors

Structure	Compound	Binding site	IC50 (μM)	Cell line/in vivo	References	Clinical trial
	Artemisinin	Leu263, Phe264, Gln267, Ile977, Ile981, Ala985, Asn1039, Leu1040, Ile1041 and Asn1042 (*)	9.6	Breast cancer	[109]	N/A
			> 40	NSCLC	[110]
			> 60	Prostate cancer	[111]
			> 60	Renal cancer
			> 60	Ovarian cancer
			12–60	Leukemia
			101–(> 1000)	Melanoma	[112]
			> 50	Neuroblastoma
			156–204	Colon cancer
			31–(> 1000)	Pancreas cancer
			9.7	HCC	[113]
	CAD204520	Asp59 (M1), Val62 (M1), Asn101 (M2), Asp254 (M3), Pro312 (M4)	2.1–9.9	T-ALL	[114]	N/A
			1.4–12.7	MCL
			N/A	T-ALL xenografted model
	Casearin J	N/A	0.7–2.5	T-ALL	[115, 116]	N/A
	Curcumin	Hydrophobic task between M3 and M5	7–15	Purified SERCA	[117]	NCT02064673 NCT04403568 NCT04266275 NCT01490996 NCT00094445
			50	Glioblastoma	[118]
			10–20	Colorectal cancer	[119]
			10–20	B-ALL	[120]
			15 ± 6.8–25 ± 5.2	Cervical cancer	[121]
			11.31 ± 1.47	Breast cancer	[122]
			5.5–11.6	HNSCC	[123]
			N/A	Liposarcoma xenografted model	[124]
	CXL017	N/A	1.04	NCI-60 cancer cell line panel	[125]	N/A
			13.5 ± 0.5	AML	[126]
	Cyclopiazonic acid	Gln56 (M1), Asp59 (M1), Asn101 (M2), hydrophobic indole group (M3, M4)	0.175	AML	[127]	N/A
			0.125	Renal carcinoma
			0.09 (SERCA1b) 2.5 (SERCA2b) 0.6 (SERCA3a)	Purified SERCA	[50]
			14.76–17.84	T-ALL	[35]
	DBHQ	Asp59 (M1), Pro308 (M4)	7 ± 4 (SERCA1b) 2.6 ± 1.3 (SERCA2b) 1.7 ± 1 (SERCA3a)	Purified SERCA	[50]	N/A
	sHA 14–1	N/A	29.2 ± 4.9 (SERCA1a) 23.5 ± 4.2 (SERCA2b)	Purified SERCA	[128]	N/A
			50	B-ALL
	Thapsigargin	Phe256 (M3); Ile765 (M5); Tyr837 (M7)	2.1 × 10–4 (SERCA1b) 1.3 × 10–3 (SERCA2b) 0.012 (SERCA3a)	Purified SERCA	[50]	N/A
			0.007 ± 0.001–3 ± 1	AML	[126]
			~4	Adrenocortical carcinoma (ACC)	[129]
			N/A	ACC xenografted model
			3.7 × 10–4-14.67	NSCLC	[35, 130]
			0.13–3.94	AML
			5.5 × 10–4-0.026	Breast cancer
			0.021	Cervix cancer
			1.7 × 10–3	Melanoma
			1.8 × 10–3-0.038	T-ALL
			7.8 × 10–3-0.011	Prostate cancer
			N/A	Drosophila intestinal stem cell model
			N/A	T-ALL xenografted model

^(*)The binding site of artemisinin is referred to PfATP6 on Plasmodium Falciparum based on computational analysis and docking simulations [131, 132]