Table 1 Pharmacological characteristics of the main MCL-1 inhibitors

S63845

K_i < 1.2 nM

Yes

No

Yes

Yes

Few: NSCLC, breast cancer, melanoma

AMG 176

K_i = 0.06 nM

Yes

No

Yes

Yes

Breast cancer

AZD5991

K_i = 0.2 nM

Yes

No

Yes

Yes

n/a

VU661013

K_i = 97 ± 30 pM

n/a

no

-(not at protein level)

n/a

n/a

Compound 42

K_i = 0.03 nM

n/a

n/a

Yes

Probably (> 10-fold shift in IC50 in BAX/BAK KO cells)

TNBC, but lower activity as compared to hematological tumors  (promising activity in chemotherapy combination approaches)

b-carboline copper(II) complexes

K_i = 1.2–96.4 nM

n/a

n/a

n/a

Yes

NSCLC