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Assay Detail

CHEMBL1028099

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Functional
Antiproliferative activity against human BT474 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-474
Confidence 1 — Organism
Curated By Autocuration

Target

BT-474 (CHEMBL614529)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R.
J Med Chem (2008) 51 : 5663 -5679
PubMed 18800763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.21 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494089 GSK-690693 1.0 1 7.30
CHEMBL494060 1 6.58
CHEMBL523859 1 6.44
CHEMBL1794065 GSK-554170A 1 6.42
CHEMBL453510 1 6.38
CHEMBL493269 1 6.16
CHEMBL521642 1 6.12
CHEMBL494088 1 5.99
CHEMBL1794066 GSK-619487A 1 5.89
CHEMBL522351 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494089 GSK-690693 IC50 = 50.0 nM 7.30
CHEMBL494060 IC50 = 260.0 nM 6.58
CHEMBL523859 IC50 = 360.0 nM 6.44
CHEMBL1794065 GSK-554170A IC50 = 380.0 nM 6.42
CHEMBL453510 IC50 = 420.0 nM 6.38
CHEMBL493269 IC50 = 700.0 nM 6.16
CHEMBL521642 IC50 = 760.0 nM 6.12
CHEMBL494088 IC50 = 1030.0 nM 5.99
CHEMBL1794066 GSK-619487A IC50 = 1280.0 nM 5.89
CHEMBL522351 IC50 = 14200.0 nM 4.85