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Assay Detail

CHEMBL5096372

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant His6-tagged human Bcl-xL (1 to 196 residues) expressed in Escherichia coli using biotinylated Bim BH3 peptide as substrate incubated for 60 mins by TR-FRET analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bcl-2-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology.
Li K.
Bioorg Med Chem Lett (2021) 32 : 127717 -127717
PubMed 33253879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.16 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446378 TAPOTOCLAX 1.0 1 6.16
CHEMBL4650225 MURIZATOCLAX 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446378 TAPOTOCLAX Ki = 700.0 nM 6.16
CHEMBL4650225 MURIZATOCLAX Ki > 5000.0 nM -