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Assay Detail

CHEMBL909614

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

Functional
Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type FL5.12
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.
J Med Chem (2007) 50 : 641 -662
PubMed 17256834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.10 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376408 ABT 737 1.0 1 7.30
CHEMBL376410 1 6.77
CHEMBL376409 1 6.44
CHEMBL384218 1 6.41
CHEMBL217960 1 6.18
CHEMBL218408 1 5.96
CHEMBL374309 1 5.89
CHEMBL218524 1 5.72
CHEMBL384217 1 5.48
CHEMBL192571 1 4.89
CHEMBL266944 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376408 ABT 737 EC50 = 50.0 nM 7.30
CHEMBL376410 EC50 = 170.0 nM 6.77
CHEMBL376409 EC50 = 360.0 nM 6.44
CHEMBL384218 EC50 = 390.0 nM 6.41
CHEMBL217960 EC50 = 660.0 nM 6.18
CHEMBL218408 EC50 = 1100.0 nM 5.96
CHEMBL374309 EC50 = 1300.0 nM 5.89
CHEMBL218524 EC50 = 1900.0 nM 5.72
CHEMBL384217 EC50 = 3300.0 nM 5.48
CHEMBL192571 EC50 = 13000.0 nM 4.89
CHEMBL266944 EC50 > 20000.0 nM -