Table 2.

MCL-1 targeted anti-tumor drugs in the preclinical stage

Compound		Efficacy towards malignant cells	In vitro potency	drug discovery method	References
MIM1		MCL-1 dependent leukemia cells	IC50: < 4.2 μM	HTS (2013)	[81]
UMI-59/77		BxPC-3 xenograft model	Ki: 490 nM	HTS (2014)	[84]
Complex 39		NCI-H460 cell line and xenograft model	IC50: 12–18 μM		[102]
Complex 14		NCI-H460 xenograft model	Ki: 1.4 nM		[101]
Pyridoclax/Compound12		Ovarian cancer cell line	–	(2014/2018)	[77, 78]
ML311/EU-5346		Active MCL-1 cell line	IC50: 0.31 μM	HTS (2013)	[82, 83]
A-1210477		MCL-1-dependent cell lines	Ki: 4–5 nM	HTS (2015)	[62]
BIM SAHBA	NA	DLBCL cell lines	EC50: 2–18 μM		[79]
MS1	PREIWMTQGLRRLGDEINAYYAR	MCL-1 dependent cell lines	Kd:1.9 ± 1.0 nM		[80]
VU661013		AML, MM, triple negative breast cancer cell lines	Ki: 97 ± 30 pM	Structure-based design (2018)	[90, 124]
Wang.Compound12		NCI-H345 cell line	IC50: 2.2 μM	Fragment-based approach (2016)	[107]
Compound8		A2780, MCF-7, SMMC-7721 and DLD1 cell lines	IC50: 38–47 μM	Virtual screening (2017)	[108]
Compound24		Lymphoma cell lines	Ki: 100 nM	HTS and virtual screening (2020)	[109]
Compound M08		Hematological and solid cancer cell lines	Ki: 0.53 ± 0.07 μM	Structure-based virtual screening (2020)	[110]
Compound5		L-363, LP-1, NCI-H929 and MOLP-8	IC50: 3.4 nM		[92]
C3		HeLa, K562, NCI-H23 cell line	IC50: 0.78 ± 0.12 μM	(2019)	[105]
dMCL1-2		MM cell line OPM2	Kd: 30 nM	(2019)	[104]
MI-223		H1299 cell	Kd: 193 ± 4.3 nM	Virtual screening (2018)	[91]
APG-3526	NA	MM cell line	IC50: 7 nM	(2020)	[106]

EC₅₀ Half-maximal concentration of drug, IC₅₀ Concentration inhibitory to 50% of cells, K_i Inhibition constant, K_d Dissociation constant