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Assay Detail

CHEMBL949293

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

Binding
Inhibition of human KDR phosphorylation in mouse NIH3T3 cells by ELISA
34
Total Activities
34
Compounds Tested
2
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

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.
Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR.
J Med Chem (2008) 51 : 1231 -1241
PubMed 18260617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.44 8.52
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409349 1 8.52
CHEMBL410130 1 8.30
CHEMBL272802 1 8.30
CHEMBL269894 1 7.96
CHEMBL271170 1 7.89
CHEMBL271381 1 7.82
CHEMBL272183 1 7.77
CHEMBL269884 1 7.75
CHEMBL273077 1 7.72
CHEMBL270084 1 7.70
CHEMBL270086 1 7.68
CHEMBL406404 1 7.66
CHEMBL406660 1 7.64
CHEMBL411725 1 7.60
CHEMBL271600 1 7.55
CHEMBL430090 1 7.51
CHEMBL270506 1 7.50
CHEMBL272453 1 7.44
CHEMBL260307 1 7.41
CHEMBL410664 1 7.40
CHEMBL272645 1 7.36
CHEMBL271796 1 7.19
CHEMBL271386 1 7.10
CHEMBL269862 1 7.09
CHEMBL410663 1 7.03
CHEMBL269885 1 6.97
CHEMBL271955 1 6.91
CHEMBL269886 1 6.76
CHEMBL273048 1 6.75
CHEMBL410504 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409349 IC50 = 3.0 nM 8.52
CHEMBL410130 IC50 = 5.0 nM 8.30
CHEMBL272802 IC50 = 5.0 nM 8.30
CHEMBL269894 IC50 = 11.0 nM 7.96
CHEMBL271170 IC50 = 13.0 nM 7.89
CHEMBL271381 IC50 = 15.0 nM 7.82
CHEMBL272183 IC50 = 17.0 nM 7.77
CHEMBL269884 IC50 = 18.0 nM 7.75
CHEMBL273077 IC50 = 19.0 nM 7.72
CHEMBL270084 IC50 = 20.0 nM 7.70
CHEMBL270086 IC50 = 21.0 nM 7.68
CHEMBL406404 IC50 = 22.0 nM 7.66
CHEMBL406660 IC50 = 23.0 nM 7.64
CHEMBL411725 IC50 = 25.0 nM 7.60
CHEMBL271600 IC50 = 28.0 nM 7.55
CHEMBL430090 IC50 = 31.0 nM 7.51
CHEMBL270506 IC50 = 32.0 nM 7.50
CHEMBL272453 IC50 = 36.0 nM 7.44
CHEMBL260307 IC50 = 39.0 nM 7.41
CHEMBL410664 IC50 = 40.0 nM 7.40
CHEMBL272645 IC50 = 44.0 nM 7.36
CHEMBL271796 IC50 = 65.0 nM 7.19
CHEMBL271386 IC50 = 80.0 nM 7.10
CHEMBL269862 IC50 = 81.0 nM 7.09
CHEMBL410663 IC50 = 94.0 nM 7.03
CHEMBL269885 IC50 = 106.0 nM 6.97
CHEMBL271955 IC50 = 123.0 nM 6.91
CHEMBL269886 IC50 = 173.0 nM 6.76
CHEMBL273048 IC50 = 179.0 nM 6.75
CHEMBL410504 IC50 = 497.0 nM 6.30
CHEMBL409912 IC50 = 1000.0 nM 6.00
CHEMBL270489 Activity - -
CHEMBL270302 Activity - -
CHEMBL260305 Activity - -