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Assay Detail

CHEMBL1018146

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

Binding
Inhibition of GST-IGF1R
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Miller LM, Mayer SC, Berger DM, Boschelli DH, Boschelli F, Di L, Du X, Dutia M, Floyd MB, Johnson M, Kenny CH, Krishnamurthy G, Moy F, Petusky S, Tkach D, Torres N, Wu B, Xu W.
Bioorg Med Chem Lett (2009) 19 : 62 -66
PubMed 19041240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 7.16 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447167 1 8.05
CHEMBL461662 1 8.00
CHEMBL453681 1 7.96
CHEMBL505519 1 7.89
CHEMBL512412 1 7.85
CHEMBL447951 1 7.85
CHEMBL498816 1 7.82
CHEMBL499661 1 7.80
CHEMBL504954 1 7.80
CHEMBL442912 1 7.77
CHEMBL504929 1 7.70
CHEMBL503167 1 7.70
CHEMBL457421 1 7.62
CHEMBL504379 1 7.58
CHEMBL467438 1 7.58
CHEMBL468700 1 7.52
CHEMBL469294 1 7.52
CHEMBL469295 1 7.51
CHEMBL448967 1 7.50
CHEMBL448243 1 7.35
CHEMBL501359 1 7.33
CHEMBL103045 1 7.30
CHEMBL463619 1 7.19
CHEMBL318804 1 7.18
CHEMBL502423 1 7.17
CHEMBL460377 1 7.10
CHEMBL323515 1 7.06
CHEMBL507862 1 6.87
CHEMBL460164 1 6.85
CHEMBL512088 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447167 IC50 = 9.0 nM 8.05
CHEMBL461662 IC50 = 10.0 nM 8.00
CHEMBL453681 IC50 = 11.0 nM 7.96
CHEMBL505519 IC50 = 13.0 nM 7.89
CHEMBL512412 IC50 = 14.0 nM 7.85
CHEMBL447951 IC50 = 14.0 nM 7.85
CHEMBL498816 IC50 = 15.0 nM 7.82
CHEMBL499661 IC50 = 16.0 nM 7.80
CHEMBL504954 IC50 = 16.0 nM 7.80
CHEMBL442912 IC50 = 17.0 nM 7.77
CHEMBL503167 IC50 = 20.0 nM 7.70
CHEMBL504929 IC50 = 20.0 nM 7.70
CHEMBL457421 IC50 = 24.0 nM 7.62
CHEMBL504379 IC50 = 26.0 nM 7.58
CHEMBL467438 IC50 = 26.0 nM 7.58
CHEMBL468700 IC50 = 30.0 nM 7.52
CHEMBL469294 IC50 = 30.0 nM 7.52
CHEMBL469295 IC50 = 31.0 nM 7.51
CHEMBL448967 IC50 = 32.0 nM 7.50
CHEMBL448243 IC50 = 45.0 nM 7.35
CHEMBL501359 IC50 = 47.0 nM 7.33
CHEMBL103045 IC50 = 50.0 nM 7.30
CHEMBL463619 IC50 = 65.0 nM 7.19
CHEMBL318804 IC50 = 66.0 nM 7.18
CHEMBL502423 IC50 = 67.0 nM 7.17
CHEMBL460377 IC50 = 79.0 nM 7.10
CHEMBL323515 IC50 = 88.0 nM 7.06
CHEMBL507862 IC50 = 135.0 nM 6.87
CHEMBL460164 IC50 = 140.0 nM 6.85
CHEMBL512088 IC50 = 150.0 nM 6.82
CHEMBL512813 IC50 = 151.0 nM 6.82
CHEMBL460165 IC50 = 189.0 nM 6.72
CHEMBL447581 IC50 = 291.0 nM 6.54
CHEMBL468907 IC50 = 394.0 nM 6.41
CHEMBL467232 IC50 = 600.0 nM 6.22
CHEMBL468269 IC50 = 847.0 nM 6.07
CHEMBL322857 IC50 = 1000.0 nM 6.00
CHEMBL461015 IC50 = 1090.0 nM 5.96
CHEMBL443410 IC50 = 3880.0 nM 5.41
CHEMBL444223 IC50 = 13700.0 nM 4.86
CHEMBL318326 IC50 > 10000.0 nM -