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Assay Detail

CHEMBL1670374

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

Binding
Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy.
Jin M, Kleinberg A, Cooke A, Gokhale PC, Foreman K, Dong H, Siu KW, Bittner MA, Mulvihill KM, Yao Y, Landfair D, O'Connor M, Mak G, Pachter JA, Wild R, Rosenfeld-Franklin M, Ji Q, Mulvihill MJ.
Bioorg Med Chem Lett (2011) 21 : 1176 -1180
PubMed 21251824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1667943 1 8.70
CHEMBL1667947 1 8.40
CHEMBL1667945 1 8.30
CHEMBL1667939 1 8.30
CHEMBL1667941 1 8.30
CHEMBL1667942 1 8.30
CHEMBL1667948 1 8.22
CHEMBL1667940 1 8.22
CHEMBL1667936 1 8.10
CHEMBL1667946 1 8.10
CHEMBL1667950 1 7.85
CHEMBL1667935 1 7.77
CHEMBL249295 1 7.72
CHEMBL1667944 1 7.70
CHEMBL410659 1 7.70
CHEMBL1667949 1 7.68
CHEMBL1091644 LINSITINIB 3.0 1 7.62
CHEMBL1667938 1 7.57
CHEMBL1667937 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1667943 IC50 = 2.0 nM 8.70
CHEMBL1667947 IC50 = 4.0 nM 8.40
CHEMBL1667945 IC50 = 5.0 nM 8.30
CHEMBL1667939 IC50 = 5.0 nM 8.30
CHEMBL1667941 IC50 = 5.0 nM 8.30
CHEMBL1667942 IC50 = 5.0 nM 8.30
CHEMBL1667948 IC50 = 6.0 nM 8.22
CHEMBL1667940 IC50 = 6.0 nM 8.22
CHEMBL1667936 IC50 = 8.0 nM 8.10
CHEMBL1667946 IC50 = 8.0 nM 8.10
CHEMBL1667950 IC50 = 14.0 nM 7.85
CHEMBL1667935 IC50 = 17.0 nM 7.77
CHEMBL249295 IC50 = 19.0 nM 7.72
CHEMBL1667944 IC50 = 20.0 nM 7.70
CHEMBL410659 IC50 = 20.0 nM 7.70
CHEMBL1667949 IC50 = 21.0 nM 7.68
CHEMBL1091644 LINSITINIB IC50 = 24.0 nM 7.62
CHEMBL1667938 IC50 = 27.0 nM 7.57
CHEMBL1667937 IC50 = 285.0 nM 6.54