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Assay Detail

CHEMBL5327666

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Binding
Inhibition of human GST-tagged MUS81-ECE1 expressed in Escherichia coli BL21(DE3)Rosetta2 cells incubated for 15 mins by FRET based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

MUS81-ECE1 (CHEMBL5465380)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of small-molecule inhibitors of human MUS81-EME1/2 by FRET-based high-throughput screening.
Zhang X, Chen X, Lu L, Fang Q, Liu C, Lin Z.
Bioorg Med Chem (2023) 90 : 117383 -117383
PubMed 37352577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.91 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071130 1 6.25
CHEMBL1200976 IDARUBICIN HYDROCHLORIDE 4.0 1 6.21
CHEMBL2354444 PIRARUBICIN 3.0 1 6.10
CHEMBL5394285 1 6.00
CHEMBL4084119 LIRAGLUTIDE 4.0 1 5.93
CHEMBL5437637 1 5.90
CHEMBL449392 CORILAGIN 1 5.89
CHEMBL445177 GINGKOLIC ACID 1 5.84
CHEMBL1241028 1 5.74
CHEMBL264938 GALLOCATECHIN GALLATE 1 5.70
CHEMBL3289398 1 5.48
CHEMBL1209885 DYNASORE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071130 IC50 = 560.0 nM 6.25
CHEMBL1200976 IDARUBICIN HYDROCHLORIDE IC50 = 610.0 nM 6.21
CHEMBL2354444 PIRARUBICIN IC50 = 790.0 nM 6.10
CHEMBL5394285 IC50 = 990.0 nM 6.00
CHEMBL4084119 LIRAGLUTIDE IC50 = 1170.0 nM 5.93
CHEMBL5437637 IC50 = 1270.0 nM 5.90
CHEMBL449392 CORILAGIN IC50 = 1290.0 nM 5.89
CHEMBL445177 GINGKOLIC ACID IC50 = 1450.0 nM 5.84
CHEMBL1241028 IC50 = 1840.0 nM 5.74
CHEMBL264938 GALLOCATECHIN GALLATE IC50 = 1990.0 nM 5.70
CHEMBL3289398 IC50 = 3330.0 nM 5.48
CHEMBL1209885 DYNASORE IC50 ~ 11500.0 nM -