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Assay Detail

CHEMBL5251907

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

Functional
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Rec1
Confidence 1 — Organism
Curated By Autocuration

Target

Rec1 (CHEMBL4483266)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
Guo Y, Hu N, Liu Y, Zhang W, Yu D, Shi G, Zhang B, Yin L, Wei M, Yuan X, Luo L, Wang F, Song X, Xin L, Wei Q, Li Y, Guo Y, Chen S, Zhang T, Zhang S, Zhou X, Zhang C, Su D, Liu J, Cheng Z, Zhang J, Xing H, Sun H, Li X, Zhao Y, He M, Wu Y, Guo Y, Sun X, Tian A, Zhou C, Young S, Liu X, Wang L, Wang Z.
J Med Chem (2023) 66 : 4025 -4044
PubMed 36912866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.22 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3936761 ZANUBRUTINIB 4.0 1 9.44
CHEMBL5272404 1 8.29
CHEMBL5288751 1 8.06
CHEMBL5276374 1 7.98
CHEMBL5282956 1 7.94
CHEMBL5275348 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3936761 ZANUBRUTINIB IC50 = 0.36 nM 9.44
CHEMBL5272404 IC50 = 5.1 nM 8.29
CHEMBL5288751 IC50 = 8.7 nM 8.06
CHEMBL5276374 IC50 = 10.4 nM 7.98
CHEMBL5282956 IC50 = 11.6 nM 7.94
CHEMBL5275348 IC50 = 26.6 nM 7.58