JNJ-4355

JNJ-4355 : Inhibitor of MCL1

Structure

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Information

MCL1

Inhibitor

up to 10 uM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q07820

Target Class: Other

Target SubClass: BCL2 family

Potency: Ki

Potency Value: 0.015 nM

Potency Assay: HTRF assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Induced myeloid leukemia cell differentiation prot ...

DOI Reference: 10.1158/1538-7445.AM2022-2133

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Shows good selectivity vs the closest related protein hBCL2 (Ki > 3.75 µM) and other family members hBCL2A1 (BFL-1) (Ki > 5 µM) and hBCL2L1BCL-XL (Ki > 5 µM). Closest off-targets in the CEREP panel (76 targets) at 1 µM (% inhibition) are Cl- channel (GABA-gated) = 22.6%, hPTGS2(COX2) = 20.2%, hBZDp (TSPO) = 19,1 %.

Potency assay, off target (cells): Cell activity was tested with various cell lines (AC50 = half-maximal activity concentration). Two different assays were used : CTG = Cell titer Glo assay (Promega), CasGlo= Caspase-Glo assay (Promega). Conclusuons: There is a high cell potency across a range of hematological cancers.

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