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Assay Detail

CHEMBL3382385

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

Binding
Inhibition of BCL-XL (unknown origin) expressed in mcl-1 deficient MEF assessed as induction of cell killing incubated for 48 hrs in presence of 10% FBS by Cell titerGlo reagent based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bcl-2-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

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 8 7.28 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342195 1 8.00
CHEMBL3342196 1 7.70
CHEMBL3342192 1 7.22
CHEMBL3342194 1 6.19
CHEMBL3342189 1 -
CHEMBL3342190 1 -
CHEMBL3342191 A-1107969 1 -
CHEMBL3342193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342195 EC50 = 10.0 nM 8.00
CHEMBL3342196 EC50 = 20.0 nM 7.70
CHEMBL3342192 EC50 = 60.0 nM 7.22
CHEMBL3342194 EC50 = 640.0 nM 6.19
CHEMBL3342189 EC50 > 5000.0 nM -
CHEMBL3342190 EC50 > 5000.0 nM -
CHEMBL3342191 A-1107969 EC50 > 5000.0 nM -
CHEMBL3342193 EC50 > 5000.0 nM -