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Assay Detail

CHEMBL2345533

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

Binding
Binding affinity to his-tagged Mcl-1 R263A mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) cells by ITC analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach.
Zhang Z, Song T, Li X, Wu Z, Feng Y, Xie F, Liu C, Qin J, Chen H.
Eur J Med Chem (2013) 59 : 141 -149
PubMed 23220642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 4.46 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2333148 1 5.17
CHEMBL2333143 1 4.34
CHEMBL2314369 1 4.29
CHEMBL2333147 1 4.04
CHEMBL2333142 CYANOACETAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2333148 Kd = 6720.0 nM 5.17
CHEMBL2333143 Kd = 46170.0 nM 4.34
CHEMBL2314369 Kd = 51390.0 nM 4.29
CHEMBL2333147 Kd = 90830.0 nM 4.04
CHEMBL2333142 CYANOACETAMIDE Kd > 1000000.0 nM -