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Assay Detail

CHEMBL4044889

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

Binding
Inhibition of C-terminal biotin-labelled BCoR/wild-type BCL6 BTB domain (unknown origin) protein-protein interaction by ELISA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

BCoR-BCL6 (CHEMBL4106125)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design.
Yasui T, Yamamoto T, Sakai N, Asano K, Takai T, Yoshitomi Y, Davis M, Takagi T, Sakamoto K, Sogabe S, Kamada Y, Lane W, Snell G, Iwata M, Goto M, Inooka H, Sakamoto JI, Nakada Y, Imaeda Y.
Bioorg Med Chem (2017) 25 : 4876 -4886
PubMed 28760529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.73 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075278 1 7.00
CHEMBL4076344 1 6.89
CHEMBL4076619 1 6.89
CHEMBL4085850 1 6.89
CHEMBL4103775 1 6.82
CHEMBL4069588 1 6.66
CHEMBL4093597 1 6.62
CHEMBL4066000 1 6.37
CHEMBL4092657 1 5.37
CHEMBL4063725 1 5.35
CHEMBL4084898 1 5.07
CHEMBL4096591 1 4.85
CHEMBL4074632 1 4.37
CHEMBL4101332 1 4.21
CHEMBL1517539 1 4.16
CHEMBL4070173 1 4.08
CHEMBL4070563 1 -
CHEMBL4063249 TP-021n 1 -
CHEMBL4066375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075278 IC50 = 100.0 nM 7.00
CHEMBL4076344 IC50 = 130.0 nM 6.89
CHEMBL4076619 IC50 = 130.0 nM 6.89
CHEMBL4085850 IC50 = 130.0 nM 6.89
CHEMBL4103775 IC50 = 150.0 nM 6.82
CHEMBL4069588 IC50 = 220.0 nM 6.66
CHEMBL4093597 IC50 = 240.0 nM 6.62
CHEMBL4066000 IC50 = 430.0 nM 6.37
CHEMBL4092657 IC50 = 4300.0 nM 5.37
CHEMBL4063725 IC50 = 4500.0 nM 5.35
CHEMBL4084898 IC50 = 8600.0 nM 5.07
CHEMBL4096591 IC50 = 14000.0 nM 4.85
CHEMBL4074632 IC50 = 43000.0 nM 4.37
CHEMBL4101332 IC50 = 62000.0 nM 4.21
CHEMBL1517539 IC50 = 69000.0 nM 4.16
CHEMBL4070173 IC50 = 83000.0 nM 4.08
CHEMBL4070563 IC50 > 300000.0 nM -
CHEMBL4063249 TP-021n IC50 = 110000.0 nM -
CHEMBL4066375 IC50 = 200000.0 nM -