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Assay Detail

CHEMBL2399241

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

Binding
Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Leukemia cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G.
J Med Chem (2013) 56 : 5514 -5540
PubMed 23767404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.32 4.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2398260 1 4.40
CHEMBL2398249 1 4.38
CHEMBL2398173 1 4.17
CHEMBL2398290 1 -
CHEMBL2398263 1 -
CHEMBL2398262 1 -
CHEMBL2398170 1 -
CHEMBL2398286 1 -
CHEMBL2398292 1 -
CHEMBL376408 ABT 737 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2398260 IC50 = 40000.0 nM 4.40
CHEMBL2398249 IC50 = 42000.0 nM 4.38
CHEMBL2398173 IC50 = 68000.0 nM 4.17
CHEMBL2398290 IC50 = 110000.0 nM -
CHEMBL2398263 IC50 > 100000.0 nM -
CHEMBL2398262 IC50 > 100000.0 nM -
CHEMBL2398170 IC50 > 100000.0 nM -
CHEMBL2398286 IC50 > 100000.0 nM -
CHEMBL2398292 IC50 > 100000.0 nM -
CHEMBL376408 ABT 737 IC50 > 1000.0 nM -