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Assay Detail

CHEMBL820673

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

Binding
In vitro inhibitory concentration against VEGF receptor 2.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.
Plé PA, Green TP, Hennequin LF, Curwen J, Fennell M, Allen J, Lambert-Van Der Brempt C, Costello G.
J Med Chem (2004) 47 : 871 -887
PubMed 14761189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.48 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172518 1 7.00
CHEMBL171558 1 6.60
CHEMBL171745 1 6.39
CHEMBL355282 1 6.38
CHEMBL352992 1 6.17
CHEMBL169797 1 5.96
CHEMBL172450 1 5.93
CHEMBL352977 1 5.91
CHEMBL169643 1 5.86
CHEMBL169186 1 5.66
CHEMBL353070 1 5.63
CHEMBL171125 1 5.30
CHEMBL167890 1 5.09
CHEMBL170984 1 4.81
CHEMBL369360 1 4.77
CHEMBL173799 1 4.37
CHEMBL352877 1 4.13
CHEMBL354145 1 4.11
CHEMBL422564 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172518 IC50 = 100.0 nM 7.00
CHEMBL171558 IC50 = 250.0 nM 6.60
CHEMBL171745 IC50 = 410.0 nM 6.39
CHEMBL355282 IC50 = 420.0 nM 6.38
CHEMBL352992 IC50 = 670.0 nM 6.17
CHEMBL169797 IC50 = 1110.0 nM 5.96
CHEMBL172450 IC50 = 1180.0 nM 5.93
CHEMBL352977 IC50 = 1230.0 nM 5.91
CHEMBL169643 IC50 = 1380.0 nM 5.86
CHEMBL169186 IC50 = 2170.0 nM 5.66
CHEMBL353070 IC50 = 2320.0 nM 5.63
CHEMBL171125 IC50 = 4960.0 nM 5.30
CHEMBL167890 IC50 = 8160.0 nM 5.09
CHEMBL170984 IC50 = 15600.0 nM 4.81
CHEMBL369360 IC50 = 17030.0 nM 4.77
CHEMBL173799 IC50 = 42640.0 nM 4.37
CHEMBL352877 IC50 = 73820.0 nM 4.13
CHEMBL354145 IC50 = 77000.0 nM 4.11
CHEMBL422564 IC50 = 91350.0 nM 4.04