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Assay Detail

CHEMBL971607

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Functional
Antiproliferative activity against transgenic mouse SAL cells overexpressing human IGF1R assessed as [3H]thymidine incorporation after 72 hrs
10
Total Activities
10
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

Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D.
J Med Chem (2008) 51 : 5897 -5900
PubMed 18763755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.06 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL512126 1 7.89
CHEMBL469292 1 7.40
CHEMBL460997 1 7.34
CHEMBL468672 1 7.12
CHEMBL461198 1 7.07
CHEMBL401930 1 6.96
CHEMBL461422 1 6.79
CHEMBL459729 1 6.73
CHEMBL468671 1 6.66
CHEMBL460996 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL512126 IC50 = 13.0 nM 7.89
CHEMBL469292 IC50 = 40.0 nM 7.40
CHEMBL460997 IC50 = 46.0 nM 7.34
CHEMBL468672 IC50 = 76.0 nM 7.12
CHEMBL461198 IC50 = 85.0 nM 7.07
CHEMBL401930 IC50 = 110.0 nM 6.96
CHEMBL461422 IC50 = 162.0 nM 6.79
CHEMBL459729 IC50 = 185.0 nM 6.73
CHEMBL468671 IC50 = 217.0 nM 6.66
CHEMBL460996 IC50 = 241.0 nM 6.62