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Assay Detail

CHEMBL928516

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Binding
Inhibition of IGF1R expressed in SAL cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type SAL
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Saulnier MG, Frennesson DB, Wittman MD, Zimmermann K, Velaparthi U, Langley DR, Struzynski C, Sang X, Carboni J, Li A, Greer A, Yang Z, Balimane P, Gottardis M, Attar R, Vyas D.
Bioorg Med Chem Lett (2008) 18 : 1702 -1707
PubMed 18258427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.32 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401930 1 6.96
CHEMBL257114 1 6.84
CHEMBL257325 1 6.71
CHEMBL256495 1 6.58
CHEMBL403015 1 6.55
CHEMBL257326 1 6.54
CHEMBL256702 1 6.51
CHEMBL256072 1 6.47
CHEMBL256074 1 6.46
CHEMBL256277 1 6.44
CHEMBL401766 1 6.42
CHEMBL256703 1 6.40
CHEMBL401767 1 6.38
CHEMBL442450 1 6.35
CHEMBL256073 1 6.33
CHEMBL256275 1 6.28
CHEMBL256908 1 6.28
CHEMBL257324 1 6.27
CHEMBL256276 1 6.23
CHEMBL256494 1 6.21
CHEMBL256910 1 6.21
CHEMBL257115 1 6.16
CHEMBL402623 1 6.16
CHEMBL256909 1 6.15
CHEMBL402625 1 6.11
CHEMBL257116 1 6.10
CHEMBL404308 1 6.09
CHEMBL404307 1 5.94
CHEMBL403218 1 5.82
CHEMBL256701 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401930 IC50 = 110.0 nM 6.96
CHEMBL257114 IC50 = 144.0 nM 6.84
CHEMBL257325 IC50 = 197.0 nM 6.71
CHEMBL256495 IC50 = 266.0 nM 6.58
CHEMBL403015 IC50 = 284.0 nM 6.55
CHEMBL257326 IC50 = 292.0 nM 6.54
CHEMBL256702 IC50 = 306.0 nM 6.51
CHEMBL256072 IC50 = 336.0 nM 6.47
CHEMBL256074 IC50 = 343.0 nM 6.46
CHEMBL256277 IC50 = 365.0 nM 6.44
CHEMBL401766 IC50 = 376.0 nM 6.42
CHEMBL256703 IC50 = 397.0 nM 6.40
CHEMBL401767 IC50 = 422.0 nM 6.38
CHEMBL442450 IC50 = 451.0 nM 6.35
CHEMBL256073 IC50 = 469.0 nM 6.33
CHEMBL256275 IC50 = 521.0 nM 6.28
CHEMBL256908 IC50 = 531.0 nM 6.28
CHEMBL257324 IC50 = 542.0 nM 6.27
CHEMBL256276 IC50 = 583.0 nM 6.23
CHEMBL256494 IC50 = 622.0 nM 6.21
CHEMBL256910 IC50 = 613.0 nM 6.21
CHEMBL257115 IC50 = 697.0 nM 6.16
CHEMBL402623 IC50 = 700.0 nM 6.16
CHEMBL256909 IC50 = 711.0 nM 6.15
CHEMBL402625 IC50 = 777.0 nM 6.11
CHEMBL257116 IC50 = 796.0 nM 6.10
CHEMBL404308 IC50 = 821.0 nM 6.09
CHEMBL404307 IC50 = 1140.0 nM 5.94
CHEMBL403218 IC50 = 1510.0 nM 5.82
CHEMBL256701 IC50 = 2034.0 nM 5.69