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Assay Detail

CHEMBL1115499

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

Binding
Inhibition of IGF1R
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Insulin-like growth factor 1 receptor (CHEMBL1957)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D.
Bioorg Med Chem Lett (2010) 20 : 3182 -3185
PubMed 20399649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.33 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095439 1 7.80
CHEMBL1094165 1 7.80
CHEMBL1098395 1 7.77
CHEMBL1097358 1 7.75
CHEMBL1097426 1 7.58
CHEMBL1097425 1 7.57
CHEMBL1098712 1 7.55
CHEMBL1094458 1 7.52
CHEMBL1097357 1 7.50
CHEMBL1096089 1 7.42
CHEMBL1094457 1 7.42
CHEMBL1097982 1 7.39
CHEMBL1096717 1 7.21
CHEMBL1094164 1 7.21
CHEMBL401930 1 7.00
CHEMBL1098711 1 7.00
CHEMBL1078891 1 7.00
CHEMBL1097032 1 6.76
CHEMBL1099314 1 6.68
CHEMBL1095404 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095439 IC50 = 16.0 nM 7.80
CHEMBL1094165 IC50 = 16.0 nM 7.80
CHEMBL1098395 IC50 = 17.0 nM 7.77
CHEMBL1097358 IC50 = 18.0 nM 7.75
CHEMBL1097426 IC50 = 26.0 nM 7.58
CHEMBL1097425 IC50 = 27.0 nM 7.57
CHEMBL1098712 IC50 = 28.0 nM 7.55
CHEMBL1094458 IC50 = 30.0 nM 7.52
CHEMBL1097357 IC50 = 32.0 nM 7.50
CHEMBL1096089 IC50 = 38.0 nM 7.42
CHEMBL1094457 IC50 = 38.0 nM 7.42
CHEMBL1097982 IC50 = 41.0 nM 7.39
CHEMBL1096717 IC50 = 62.0 nM 7.21
CHEMBL1094164 IC50 = 61.0 nM 7.21
CHEMBL401930 IC50 = 100.0 nM 7.00
CHEMBL1098711 IC50 = 100.0 nM 7.00
CHEMBL1078891 IC50 = 100.0 nM 7.00
CHEMBL1097032 IC50 = 175.0 nM 6.76
CHEMBL1099314 IC50 = 210.0 nM 6.68
CHEMBL1095404 IC50 = 270.0 nM 6.57