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Assay Detail

CHEMBL4356645

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

Binding
Inhibition of recombinant C-terminal His10x-tagged human Bcl-2 (2 to 211 residues) expressed in Escherichia coli cells interaction with biotinylated human Bim (51 to 76 residues) incubated for 60 mins by HTRF assay
1
Total Activities
1
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

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
Rescourio G, Gonzalez AZ, Jabri S, Belmontes B, Moody G, Whittington D, Huang X, Caenepeel S, Cardozo M, Cheng AC, Chow D, Dou H, Jones A, Kelly RC, Li Y, Lizarzaburu M, Lo MC, Mallari R, Meleza C, Rew Y, Simonovich S, Sun D, Turcotte S, Yan X, Wong SG, Yanez E, Zancanella M, Houze J, Medina JC, Hughes PE, Brown SP.
J Med Chem (2019) 62 : 10258 -10271
PubMed 31736296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.71 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446378 TAPOTOCLAX 1.0 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446378 TAPOTOCLAX IC50 = 1930.0 nM 5.71