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Assay Detail

CHEMBL3382386

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Functional
Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum incubated for 48 hrs by Cell titerGlo reagent based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H146
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.
ACS Med Chem Lett (2014) 5 : 1088 -1093
PubMed 25313317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.87 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342333 1 7.29
CHEMBL3342332 A-1155463 1 7.19
CHEMBL3342334 1 6.90
CHEMBL3342198 1 6.75
CHEMBL3342197 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342333 EC50 = 51.0 nM 7.29
CHEMBL3342332 A-1155463 EC50 = 65.0 nM 7.19
CHEMBL3342334 EC50 = 126.0 nM 6.90
CHEMBL3342198 EC50 = 180.0 nM 6.75
CHEMBL3342197 EC50 = 600.0 nM 6.22