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Assay Detail

CHEMBL1102239

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

Functional
Antiproliferative activity against mouse Sal cells expressing human IGF-1R assessed as [3H]thymidine incorporation after 72 hrs by scintillation assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Sal
Confidence 1 — Organism
Curated By Autocuration

Publication

SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D.
Bioorg Med Chem Lett (2010) 20 : 1744 -1748
PubMed 20153189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.69 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505919 1 7.11
CHEMBL401766 1 6.96
CHEMBL1077343 1 6.65
CHEMBL1077340 1 6.55
CHEMBL401930 1 6.47
CHEMBL256072 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505919 IC50 = 77.0 nM 7.11
CHEMBL401766 IC50 = 110.0 nM 6.96
CHEMBL1077343 IC50 = 222.0 nM 6.65
CHEMBL1077340 IC50 = 279.0 nM 6.55
CHEMBL401930 IC50 = 336.0 nM 6.47
CHEMBL256072 IC50 = 376.0 nM 6.42