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Assay Detail

CHEMBL862695

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

Binding
Inhibition of poly(Glu4-Tyr)peptide phosphorylation by recombinant VEGFR2 at 10 uM ATP and in presence of 5% mouse plasma
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.
Wissner A, Floyd MB, Johnson BD, Fraser H, Ingalls C, Nittoli T, Dushin RG, Discafani C, Nilakantan R, Marini J, Ravi M, Cheung K, Tan X, Musto S, Annable T, Siegel MM, Loganzo F.
J Med Chem (2005) 48 : 7560 -7581
PubMed 16302797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 7.41 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3706842 — — 1 8.72
CHEMBL2113199 — — 1 8.66
CHEMBL2113164 — — 1 8.62
CHEMBL2113171 — — 1 8.52
CHEMBL3706826 — — 1 8.43
CHEMBL3706817 — — 1 8.32
CHEMBL2113172 — — 1 8.29
CHEMBL3706816 — — 1 8.28
CHEMBL2113184 — — 1 8.24
CHEMBL2113193 — — 1 8.13
CHEMBL3706841 — — 1 8.00
CHEMBL3706836 — — 1 7.86
CHEMBL2113163 — — 1 7.86
CHEMBL3706837 — — 1 7.78
CHEMBL2113175 — — 1 7.61
CHEMBL3706843 — — 1 7.58
CHEMBL3706834 — — 1 7.54
CHEMBL3706815 — — 1 7.53
CHEMBL3706835 — — 1 7.49
CHEMBL2113192 — — 1 7.39
CHEMBL3706814 — — 1 7.27
CHEMBL2113188 — — 1 7.24
CHEMBL3706839 — — 1 7.22
CHEMBL3706832 — — 1 7.01
CHEMBL3706830 — — 1 6.94
CHEMBL3706819 — — 1 6.93
CHEMBL200723 — — 1 6.89
CHEMBL24828 VANDETANIB 4.0 1 6.82
CHEMBL199455 — — 1 6.80
CHEMBL2113191 — — 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3706842 — IC50 = 1.9 nM 8.72
CHEMBL2113199 — IC50 = 2.2 nM 8.66
CHEMBL2113164 — IC50 = 2.4 nM 8.62
CHEMBL2113171 — IC50 = 3.0 nM 8.52
CHEMBL3706826 — IC50 = 3.7 nM 8.43
CHEMBL3706817 — IC50 = 4.8 nM 8.32
CHEMBL2113172 — IC50 = 5.1 nM 8.29
CHEMBL3706816 — IC50 = 5.2 nM 8.28
CHEMBL2113184 — IC50 = 5.8 nM 8.24
CHEMBL2113193 — IC50 = 7.4 nM 8.13
CHEMBL3706841 — IC50 = 9.9 nM 8.00
CHEMBL3706836 — IC50 = 13.7 nM 7.86
CHEMBL2113163 — IC50 = 13.9 nM 7.86
CHEMBL3706837 — IC50 = 16.5 nM 7.78
CHEMBL2113175 — IC50 = 24.8 nM 7.61
CHEMBL3706843 — IC50 = 26.1 nM 7.58
CHEMBL3706834 — IC50 = 28.7 nM 7.54
CHEMBL3706815 — IC50 = 29.6 nM 7.53
CHEMBL3706835 — IC50 = 32.5 nM 7.49
CHEMBL2113192 — IC50 = 41.0 nM 7.39
CHEMBL3706814 — IC50 = 53.5 nM 7.27
CHEMBL2113188 — IC50 = 57.4 nM 7.24
CHEMBL3706839 — IC50 = 59.7 nM 7.22
CHEMBL3706832 — IC50 = 97.3 nM 7.01
CHEMBL3706830 — IC50 = 114.7 nM 6.94
CHEMBL3706819 — IC50 = 117.8 nM 6.93
CHEMBL200723 — IC50 = 129.9 nM 6.89
CHEMBL24828 VANDETANIB IC50 = 149.8 nM 6.82
CHEMBL199455 — IC50 = 158.6 nM 6.80
CHEMBL2113191 — IC50 = 193.5 nM 6.71
CHEMBL2113182 — IC50 = 239.2 nM 6.62
CHEMBL396472 — IC50 = 256.3 nM 6.59
CHEMBL242555 — IC50 = 366.1 nM 6.44
CHEMBL3706822 — IC50 = 375.9 nM 6.42
CHEMBL3706840 — IC50 = 495.2 nM 6.30
CHEMBL2113166 — IC50 = 569.1 nM 6.25
CHEMBL2113174 — IC50 = 560.1 nM 6.25
CHEMBL3706829 — IC50 = 803.1 nM 6.09
CHEMBL3706820 — IC50 > 1000.0 nM -
CHEMBL200818 — IC50 > 1000.0 nM -
CHEMBL2113169 — IC50 > 1000.0 nM -
CHEMBL2113165 — IC50 > 1000.0 nM -
CHEMBL2113186 — IC50 > 1000.0 nM -
CHEMBL3706825 — IC50 > 1000.0 nM -
CHEMBL2113170 — IC50 > 1000.0 nM -
CHEMBL2113173 — IC50 > 1000.0 nM -
CHEMBL3706824 — IC50 > 1000.0 nM -
CHEMBL2113167 — IC50 > 20000.0 nM -
CHEMBL3706818 — IC50 > 1000.0 nM -
CHEMBL3706828 — IC50 > 1000.0 nM -