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Assay Detail

CHEMBL959243

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

Binding
Inhibition of AKT-mediated GSK3-beta phosphorylation in human BT474 cells by mechanistic assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BT-474
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Seefeld MA, Rouse MB, McNulty KC, Sun L, Wang J, Yamashita DS, Luengo JI, Zhang S, Minthorn EA, Concha NO, Heerding DA.
Bioorg Med Chem Lett (2009) 19 : 2244 -2248
PubMed 19285393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.15 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520788 1 7.30
CHEMBL469590 1 7.10
CHEMBL523586 1 7.05
CHEMBL470597 1 7.00
CHEMBL469781 1 6.92
CHEMBL482536 1 6.77
CHEMBL496690 1 6.75
CHEMBL471034 1 6.72
CHEMBL498052 1 6.66
CHEMBL470192 1 6.62
CHEMBL469591 1 6.58
CHEMBL512135 1 6.30
CHEMBL512480 1 6.25
CHEMBL470410 1 6.11
CHEMBL512858 1 6.10
CHEMBL524998 1 6.00
CHEMBL512672 1 6.00
CHEMBL512305 1 5.96
CHEMBL471059 1 5.96
CHEMBL469802 1 5.82
CHEMBL498051 1 5.72
CHEMBL470598 1 5.72
CHEMBL482537 1 5.70
CHEMBL470596 1 5.68
CHEMBL470202 1 5.60
CHEMBL472291 1 5.33
CHEMBL513019 1 5.32
CHEMBL513728 1 5.22
CHEMBL469357 1 5.22
CHEMBL470200 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520788 IC50 = 50.0 nM 7.30
CHEMBL469590 IC50 = 80.0 nM 7.10
CHEMBL523586 IC50 = 90.0 nM 7.05
CHEMBL470597 IC50 = 100.0 nM 7.00
CHEMBL469781 IC50 = 120.0 nM 6.92
CHEMBL482536 IC50 = 170.0 nM 6.77
CHEMBL496690 IC50 = 180.0 nM 6.75
CHEMBL471034 IC50 = 190.0 nM 6.72
CHEMBL498052 IC50 = 220.0 nM 6.66
CHEMBL470192 IC50 = 240.0 nM 6.62
CHEMBL469591 IC50 = 260.0 nM 6.58
CHEMBL512135 IC50 = 500.0 nM 6.30
CHEMBL512480 IC50 = 560.0 nM 6.25
CHEMBL470410 IC50 = 780.0 nM 6.11
CHEMBL512858 IC50 = 800.0 nM 6.10
CHEMBL524998 IC50 = 1000.0 nM 6.00
CHEMBL512672 IC50 = 1000.0 nM 6.00
CHEMBL512305 IC50 = 1100.0 nM 5.96
CHEMBL471059 IC50 = 1100.0 nM 5.96
CHEMBL469802 IC50 = 1500.0 nM 5.82
CHEMBL498051 IC50 = 1900.0 nM 5.72
CHEMBL470598 IC50 = 1900.0 nM 5.72
CHEMBL482537 IC50 = 2000.0 nM 5.70
CHEMBL470596 IC50 = 2100.0 nM 5.68
CHEMBL470202 IC50 = 2500.0 nM 5.60
CHEMBL472291 IC50 = 4700.0 nM 5.33
CHEMBL513019 IC50 = 4800.0 nM 5.32
CHEMBL513728 IC50 = 6000.0 nM 5.22
CHEMBL469357 IC50 = 6000.0 nM 5.22
CHEMBL470200 IC50 = 10000.0 nM 5.00
CHEMBL470620 IC50 > 10000.0 nM -
CHEMBL512148 IC50 > 10000.0 nM -
CHEMBL470409 IC50 > 10000.0 nM -
CHEMBL469561 IC50 > 10000.0 nM -
CHEMBL469560 IC50 > 10000.0 nM -