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Assay Detail

CHEMBL1022736

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

Binding
Inhibition of IGF1R in mouse SAL cells assessed as thymidine incorporation
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type SAL
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Insulin-like growth factor 1 receptor (CHEMBL5381)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Langley DR, Sang X, Frennesson D, Carboni J, Li A, Greer A, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Vyas D.
Bioorg Med Chem Lett (2008) 18 : 4075 -4080
PubMed 18572407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.00 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521271 1 7.41
CHEMBL482089 1 7.26
CHEMBL480966 1 7.18
CHEMBL505919 1 7.11
CHEMBL520419 1 7.10
CHEMBL454467 1 7.10
CHEMBL502092 1 7.08
CHEMBL474469 1 7.07
CHEMBL451331 1 7.06
CHEMBL519300 1 7.04
CHEMBL482088 1 7.00
CHEMBL459118 1 7.00
CHEMBL506169 1 6.98
CHEMBL482126 1 6.97
CHEMBL480965 1 6.97
CHEMBL482102 1 6.97
CHEMBL401930 1 6.96
CHEMBL450610 1 6.94
CHEMBL482101 1 6.92
CHEMBL505652 1 6.89
CHEMBL510298 1 6.86
CHEMBL499584 1 6.84
CHEMBL454515 1 6.82
CHEMBL519132 1 6.81
CHEMBL502778 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521271 IC50 = 39.0 nM 7.41
CHEMBL482089 IC50 = 55.0 nM 7.26
CHEMBL480966 IC50 = 66.0 nM 7.18
CHEMBL505919 IC50 = 77.0 nM 7.11
CHEMBL520419 IC50 = 79.0 nM 7.10
CHEMBL454467 IC50 = 80.0 nM 7.10
CHEMBL502092 IC50 = 83.0 nM 7.08
CHEMBL474469 IC50 = 86.0 nM 7.07
CHEMBL451331 IC50 = 88.0 nM 7.06
CHEMBL519300 IC50 = 92.0 nM 7.04
CHEMBL482088 IC50 = 99.0 nM 7.00
CHEMBL459118 IC50 = 99.0 nM 7.00
CHEMBL506169 IC50 = 105.0 nM 6.98
CHEMBL482126 IC50 = 108.0 nM 6.97
CHEMBL480965 IC50 = 107.0 nM 6.97
CHEMBL482102 IC50 = 108.0 nM 6.97
CHEMBL401930 IC50 = 110.0 nM 6.96
CHEMBL450610 IC50 = 115.0 nM 6.94
CHEMBL482101 IC50 = 121.0 nM 6.92
CHEMBL505652 IC50 = 130.0 nM 6.89
CHEMBL510298 IC50 = 139.0 nM 6.86
CHEMBL499584 IC50 = 145.0 nM 6.84
CHEMBL454515 IC50 = 151.0 nM 6.82
CHEMBL519132 IC50 = 155.0 nM 6.81
CHEMBL502778 IC50 = 193.0 nM 6.71