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Assay Detail

CHEMBL1768789

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Functional
Antiproliferative activity against human HEL 92.1.7 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEL
Confidence 1 — Organism
Curated By Autocuration

Target

HEL (CHEMBL613888)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM.
J Med Chem (2011) 54 : 1871 -1895
PubMed 21341675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.79 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1765738 1 4.92
CHEMBL1765744 1 4.80
CHEMBL1614777 1 4.75
CHEMBL1765750 1 4.75
CHEMBL1765743 1 4.72
CHEMBL1765740 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1765738 IC50 = 12000.0 nM 4.92
CHEMBL1765744 IC50 = 16000.0 nM 4.80
CHEMBL1614777 IC50 = 18000.0 nM 4.75
CHEMBL1765750 IC50 = 18000.0 nM 4.75
CHEMBL1765743 IC50 = 19000.0 nM 4.72
CHEMBL1765740 IC50 > 30000.0 nM -