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Assay Detail

CHEMBL4378468

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

Binding
Inhibition of N-terminal GST-tagged-Mcl1 (E171 to G327) (unknown origin) expressed in Escherichia coli using HyLite Fluor 647-labeled Bim peptide C as substrate incubated for 120 to 180 mins by TR-FRET assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Hot-Spots of Mcl-1 Protein.
Denis C, Sopková-de Oliveira Santos J, Bureau R, Voisin-Chiret AS.
J Med Chem (2020) 63 : 928 -943
PubMed 31580668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.67 7.38
Ki 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297482 AZD-5991 1.0 1 9.70
CHEMBL4443085 1 7.38
CHEMBL3417691 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297482 AZD-5991 Ki = 0.2 nM 9.70
CHEMBL4443085 IC50 = 42.0 nM 7.38
CHEMBL3417691 IC50 = 1100.0 nM 5.96