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Assay Detail

CHEMBL4387152

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

Functional
Antiproliferative activity against human BT549 cells assessed as reduction in DNA replication incubated for 16 hours followed by addition of EdU and incubated for 8 hours by Alexa flour488 and HCS dye-based fluorescence imaging method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-549
Confidence 1 — Organism
Curated By Autocuration

Target

BT-549 (CHEMBL614072)
Type CELL-LINE
Organism Homo sapiens

Publication

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP.
Bioorg Med Chem Lett (2019) 29 : 2294 -2301
PubMed 31307887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.41 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4440980 1 5.70
CHEMBL4545456 1 5.68
CHEMBL4520067 1 5.58
CHEMBL4539133 1 5.46
CHEMBL4589135 1 5.29
CHEMBL4546255 1 4.77
CHEMBL4466797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4440980 EC50 = 2000.0 nM 5.70
CHEMBL4545456 EC50 = 2100.0 nM 5.68
CHEMBL4520067 EC50 = 2600.0 nM 5.58
CHEMBL4539133 EC50 = 3500.0 nM 5.46
CHEMBL4589135 EC50 = 5100.0 nM 5.29
CHEMBL4546255 EC50 = 17000.0 nM 4.77
CHEMBL4466797 EC50 > 2200.0 nM -