From: Targeting MCL-1 in cancer: current status and perspectives
Compound | Â | 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: 490Â 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: 1.4Â nM | Â | [101] |
Pyridoclax/Compound12 |
| Ovarian cancer cell line | – | (2014/2018) | |
ML311/EU-5346 |
| Active MCL-1 cell line | IC50: 0.31 μM | HTS (2013) | |
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) | |
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: 100Â 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: 3.4Â nM | Â | [92] |
C3 |
| HeLa, K562, NCI-H23 cell line | IC50: 0.78 ± 0.12 μM | (2019) | [105] |
dMCL1-2 |
| MM cell line OPM2 | Kd: 30Â nM | (2019) | [104] |
MI-223 |
| H1299 cell | Kd: 193 ± 4.3 nM | Virtual screening (2018) | [91] |
APG-3526 | NA | MM cell line | IC50: 7Â nM | (2020) | [106] |