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Assay Detail

CHEMBL1273077

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Binding
Inhibition of N-terminal FITC BH3 peptide binding to GST-tagged Bfl1 by time resolved-FRET assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Bcl-2-related protein A1 (CHEMBL6044)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of Bfl-1 with N-aryl maleimides.
Cashman JR, MacDonald M, Ghirmai S, Okolotowicz KJ, Sergienko E, Brown B, Garcia X, Zhai D, Dahl R, Reed JC.
Bioorg Med Chem Lett (2010) 20 : 6560 -6564
PubMed 20933419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.70 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1269202 1 6.40
CHEMBL1272154 1 6.40
CHEMBL1271993 1 6.35
CHEMBL1272100 1 6.21
CHEMBL1271495 1 6.16
CHEMBL1272047 1 6.10
CHEMBL1271764 1 6.10
CHEMBL1271825 1 6.00
CHEMBL1271994 1 6.00
CHEMBL1272048 1 5.96
CHEMBL1271881 1 5.92
CHEMBL1272313 1 5.89
CHEMBL1271766 1 5.85
CHEMBL1271765 1 5.72
CHEMBL1272049 1 5.70
CHEMBL1271494 1 5.68
CHEMBL1271823 1 5.58
CHEMBL1272099 1 5.48
CHEMBL1271883 1 5.41
CHEMBL1272155 1 5.39
CHEMBL1272210 1 5.30
CHEMBL1272209 1 5.21
CHEMBL1272263 1 5.08
CHEMBL1271882 1 4.97
CHEMBL1271824 1 4.96
CHEMBL1271936 1 4.45
CHEMBL1271992 1 -
CHEMBL1271938 1 -
CHEMBL1272264 1 -
CHEMBL1272312 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1269202 IC50 = 400.0 nM 6.40
CHEMBL1272154 IC50 = 400.0 nM 6.40
CHEMBL1271993 IC50 = 450.0 nM 6.35
CHEMBL1272100 IC50 = 620.0 nM 6.21
CHEMBL1271495 IC50 = 690.0 nM 6.16
CHEMBL1272047 IC50 = 800.0 nM 6.10
CHEMBL1271764 IC50 = 800.0 nM 6.10
CHEMBL1271825 IC50 = 1000.0 nM 6.00
CHEMBL1271994 IC50 = 1000.0 nM 6.00
CHEMBL1272048 IC50 = 1100.0 nM 5.96
CHEMBL1271881 IC50 = 1200.0 nM 5.92
CHEMBL1272313 IC50 = 1300.0 nM 5.89
CHEMBL1271766 IC50 = 1400.0 nM 5.85
CHEMBL1271765 IC50 = 1900.0 nM 5.72
CHEMBL1272049 IC50 = 2000.0 nM 5.70
CHEMBL1271494 IC50 = 2100.0 nM 5.68
CHEMBL1271823 IC50 = 2600.0 nM 5.58
CHEMBL1272099 IC50 = 3300.0 nM 5.48
CHEMBL1271883 IC50 = 3900.0 nM 5.41
CHEMBL1272155 IC50 = 4100.0 nM 5.39
CHEMBL1272210 IC50 = 5000.0 nM 5.30
CHEMBL1272209 IC50 = 6200.0 nM 5.21
CHEMBL1272263 IC50 = 8300.0 nM 5.08
CHEMBL1271882 IC50 = 10800.0 nM 4.97
CHEMBL1271824 IC50 = 11100.0 nM 4.96
CHEMBL1271936 IC50 = 35600.0 nM 4.45
CHEMBL1271992 IC50 > 50000.0 nM -
CHEMBL1271938 IC50 > 50000.0 nM -
CHEMBL1272264 IC50 > 10000.0 nM -
CHEMBL1272312 IC50 > 10000.0 nM -
CHEMBL1271937 IC50 > 50000.0 nM -
CHEMBL1269201 IC50 > 50000.0 nM -
CHEMBL1269036 IC50 > 10000.0 nM -
CHEMBL1271547 IC50 > 10000.0 nM -