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Assay Detail

CHEMBL3789400

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

Binding
Inhibition of IGF-1 receptor (unknown origin)
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
Stauffer F, Cowan-Jacob SW, Scheufler C, Furet P.
Bioorg Med Chem Lett (2016) 26 : 2065 -2067
PubMed 26951750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.50 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786567 1 8.05
CHEMBL3785273 1 7.22
CHEMBL1614712 1 7.21
CHEMBL3787614 1 7.10
CHEMBL3786383 1 7.10
CHEMBL3786793 1 6.96
CHEMBL3787668 1 6.89
CHEMBL3786598 1 6.80
CHEMBL3786472 1 6.58
CHEMBL3785927 1 6.51
CHEMBL3786115 1 6.43
CHEMBL3787112 1 6.38
CHEMBL3785169 1 6.31
CHEMBL3787399 1 6.26
CHEMBL3786668 1 6.20
CHEMBL3786564 1 6.08
CHEMBL3787253 1 5.72
CHEMBL3787579 1 5.70
CHEMBL3785519 1 5.43
CHEMBL3787474 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786567 IC50 = 9.0 nM 8.05
CHEMBL3785273 IC50 = 60.0 nM 7.22
CHEMBL1614712 IC50 = 61.0 nM 7.21
CHEMBL3787614 IC50 = 80.0 nM 7.10
CHEMBL3786383 IC50 = 80.0 nM 7.10
CHEMBL3786793 IC50 = 110.0 nM 6.96
CHEMBL3787668 IC50 = 130.0 nM 6.89
CHEMBL3786598 IC50 = 160.0 nM 6.80
CHEMBL3786472 IC50 = 260.0 nM 6.58
CHEMBL3785927 IC50 = 310.0 nM 6.51
CHEMBL3786115 IC50 = 370.0 nM 6.43
CHEMBL3787112 IC50 = 420.0 nM 6.38
CHEMBL3785169 IC50 = 490.0 nM 6.31
CHEMBL3787399 IC50 = 550.0 nM 6.26
CHEMBL3786668 IC50 = 630.0 nM 6.20
CHEMBL3786564 IC50 = 840.0 nM 6.08
CHEMBL3787253 IC50 = 1900.0 nM 5.72
CHEMBL3787579 IC50 = 2000.0 nM 5.70
CHEMBL3785519 IC50 = 3700.0 nM 5.43
CHEMBL3787474 IC50 = 7900.0 nM 5.10