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Assay Detail

CHEMBL3266887

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

Binding
Binding affinity to His-tagged MCL1 (171 to 327) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of MCL1-N-terminal biotin-labeled BIM BH3 peptide interaction after 30 mins by surface plasmon resonance analysis
46
Total Activities
46
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

Publication

3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
Abulwerdi FA, Liao C, Mady AS, Gavin J, Shen C, Cierpicki T, Stuckey JA, Showalter HD, Nikolovska-Coleska Z.
J Med Chem (2014) 57 : 4111 -4133
PubMed 24749893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 5.14 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3265297 1 6.06
CHEMBL3265300 1 6.05
CHEMBL3265298 1 6.04
CHEMBL3265299 1 5.84
CHEMBL3265313 1 5.82
CHEMBL3265294 1 5.69
CHEMBL3265295 1 5.64
CHEMBL1331211 1 5.62
CHEMBL1564699 1 5.57
CHEMBL3235895 1 5.56
CHEMBL3265310 1 5.41
CHEMBL3235886 1 5.40
CHEMBL3260033 1 5.30
CHEMBL1888104 1 5.30
CHEMBL3265292 1 5.21
CHEMBL2030270 1 5.15
CHEMBL1465938 1 5.14
CHEMBL3265293 1 5.12
CHEMBL3265290 1 5.06
CHEMBL1607263 1 5.06
CHEMBL3265303 1 5.02
CHEMBL3265291 1 5.01
CHEMBL3265296 1 5.00
CHEMBL3265311 1 4.96
CHEMBL1868007 1 4.94
CHEMBL1865517 1 4.90
CHEMBL3265309 1 4.83
CHEMBL3265301 1 4.79
CHEMBL3265305 1 4.74
CHEMBL3265312 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3265297 IC50 = 880.0 nM 6.06
CHEMBL3265300 IC50 = 900.0 nM 6.05
CHEMBL3265298 IC50 = 920.0 nM 6.04
CHEMBL3265299 IC50 = 1450.0 nM 5.84
CHEMBL3265313 IC50 = 1500.0 nM 5.82
CHEMBL3265294 IC50 = 2030.0 nM 5.69
CHEMBL3265295 IC50 = 2310.0 nM 5.64
CHEMBL1331211 IC50 = 2400.0 nM 5.62
CHEMBL1564699 IC50 = 2700.0 nM 5.57
CHEMBL3235895 IC50 = 2760.0 nM 5.56
CHEMBL3265310 IC50 = 3870.0 nM 5.41
CHEMBL3235886 IC50 = 4000.0 nM 5.40
CHEMBL1888104 IC50 = 5010.0 nM 5.30
CHEMBL3260033 IC50 = 5030.0 nM 5.30
CHEMBL3265292 IC50 = 6180.0 nM 5.21
CHEMBL2030270 IC50 = 7120.0 nM 5.15
CHEMBL1465938 IC50 = 7170.0 nM 5.14
CHEMBL3265293 IC50 = 7500.0 nM 5.12
CHEMBL3265290 IC50 = 8730.0 nM 5.06
CHEMBL1607263 IC50 = 8680.0 nM 5.06
CHEMBL3265303 IC50 = 9590.0 nM 5.02
CHEMBL3265291 IC50 = 9680.0 nM 5.01
CHEMBL3265296 IC50 = 9900.0 nM 5.00
CHEMBL3265311 IC50 = 10950.0 nM 4.96
CHEMBL1868007 IC50 = 11570.0 nM 4.94
CHEMBL1865517 IC50 = 12580.0 nM 4.90
CHEMBL3265309 IC50 = 14880.0 nM 4.83
CHEMBL3265301 IC50 = 16200.0 nM 4.79
CHEMBL3265305 IC50 = 18270.0 nM 4.74
CHEMBL3265312 IC50 = 19680.0 nM 4.71
CHEMBL3260041 IC50 = 26840.0 nM 4.57
CHEMBL3265304 IC50 = 30200.0 nM 4.52
CHEMBL3259874 IC50 = 45080.0 nM 4.35
CHEMBL3260039 IC50 = 58430.0 nM 4.23
CHEMBL3265306 IC50 = 63770.0 nM 4.20
CHEMBL3260034 IC50 = 64900.0 nM 4.19
CHEMBL3260040 IC50 > 100000.0 nM -
CHEMBL3260038 IC50 > 100000.0 nM -
CHEMBL3265302 IC50 > 100000.0 nM -
CHEMBL3260037 IC50 > 100000.0 nM -
CHEMBL3260036 IC50 > 100000.0 nM -
CHEMBL3260035 IC50 > 100000.0 nM -
CHEMBL3260032 IC50 - -
CHEMBL3265308 IC50 > 100000.0 nM -
CHEMBL3265307 IC50 > 100000.0 nM -
CHEMBL3265289 IC50 > 100000.0 nM -