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Assay Detail

CHEMBL3375807

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

Binding
Inhibition of KDR (unknown origin)
9
Total Activities
9
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

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

Publication

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP.
J Med Chem (2014) 57 : 10176 -10191
PubMed 25383627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.09 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354187 1 7.92
CHEMBL3354186 1 6.66
CHEMBL3354185 1 5.87
CHEMBL3354191 1 5.78
CHEMBL3354188 1 5.70
CHEMBL3354192 1 5.65
CHEMBL3354189 1 5.64
CHEMBL3352835 1 5.48
CHEMBL3354190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354187 IC50 = 12.0 nM 7.92
CHEMBL3354186 IC50 = 219.0 nM 6.66
CHEMBL3354185 IC50 = 1360.0 nM 5.87
CHEMBL3354191 IC50 = 1660.0 nM 5.78
CHEMBL3354188 IC50 = 1990.0 nM 5.70
CHEMBL3354192 IC50 = 2240.0 nM 5.65
CHEMBL3354189 IC50 = 2270.0 nM 5.64
CHEMBL3352835 IC50 = 3290.0 nM 5.48
CHEMBL3354190 IC50 > 10000.0 nM -