Assay Detail

CHEMBL4387155

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Functional

Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay

ChEMBL ↗

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Target

U-87 MG (CHEMBL614247) ↗

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U-87 MG (CHEMBL614247) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target U-87 MG

CHEMBL614247

Anchored from Assay target.

Protein identity U-87 MG

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	U-87MG ATCC
Confidence	1 — Organism
Curated By	Autocuration

Target

U-87 MG (CHEMBL614247) ↗

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	3	6.72	6.92

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3301610	ABEMACICLIB	4.0	1	6.92
CHEMBL4545456	—	—	1	6.77
CHEMBL4440980	—	—	1	6.46

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3301610	ABEMACICLIB	EC50	=	120.0	nM	6.92
CHEMBL4545456	—	EC50	=	170.0	nM	6.77
CHEMBL4440980	—	EC50	=	350.0	nM	6.46