A-1210477

BH3 mimetic of MCL1

Structure

Information

Protein target names: MCL1

Mechanism of action: BH3 mimetic

Recommended in-cell concentration:
Up to 3 uM

In Vitro Validations

Uniprot ID: Q07820
Target Class: Other
Target SubClass: BCL2 family
Potency: Ki
Potency Value: 0.454 nM
Potency Assay: Time-resolved Flourescence resonance energy transfer (TR-FRET) binding assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes, some. Several related compounds were reported in the original paper.
Target aliases:
Induced myeloid leukemia cell differentiation prot ...

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

One might have expected rodent data on A-1210477 to have appeared by now, suggesting the experiments may not have worked. For cell-line studies, some of the less active analogues in PMID 25679114 would be useful specificity controls. Note, covalent probes for the same target have been reported in PMID: 27595327

(last updated: 13 Apr 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

There are much better probes for MCL-1 now available with significantly better cell potency and demonstrated in vivo efficacy, such as AMG-176 (disclosed in 2017 AACR and ACS; Ki = 50 pM), AZD5991 (disclosed in 2017 AACR; Ki = 130 pM), and S63845 (disclosed in 2016 Nature paper; Ki ~ 1 nM).  I would not nominate A-1210477, as the other compounds are substantially better.

(last updated: 17 Apr 2017 )

SERP Ratings

In Cell Rating

(last updated: 20 Apr 2017 )