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Assay Detail

CHEMBL950174

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

Binding
Inhibition of KDR by HTRF assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
La DS, Belzile J, Bready JV, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn JC, Flynn SR, Graceffa RF, Harriman SP, Larrow JF, Long AM, Martin MW, Morrison MJ, Patel VF, Roveto PM, Wang L, Weiss MM, Whittington DA, Teffera Y, Zhao Z, Polverino AJ, Harmange JC.
J Med Chem (2008) 51 : 1695 -1705
PubMed 18311900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.33 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429743 1 10.52
CHEMBL411630 1 9.70
CHEMBL270954 1 9.30
CHEMBL270548 1 9.30
CHEMBL409867 1 9.22
CHEMBL272878 1 9.00
CHEMBL270058 1 9.00
CHEMBL270057 1 9.00
CHEMBL429430 1 9.00
CHEMBL272875 1 9.00
CHEMBL270306 1 9.00
CHEMBL272822 1 8.52
CHEMBL270550 1 7.72
CHEMBL272170 1 7.58
CHEMBL270093 1 7.58
CHEMBL272609 1 7.40
CHEMBL270545 1 7.40
CHEMBL409933 1 7.40
CHEMBL272874 1 7.28
CHEMBL405040 1 7.24
CHEMBL272688 1 7.21
CHEMBL270953 1 7.11
CHEMBL271960 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429743 IC50 = 0.03 nM 10.52
CHEMBL411630 IC50 = 0.2 nM 9.70
CHEMBL270954 IC50 = 0.5 nM 9.30
CHEMBL270548 IC50 = 0.5 nM 9.30
CHEMBL409867 IC50 = 0.6 nM 9.22
CHEMBL272878 IC50 = 1.0 nM 9.00
CHEMBL270058 IC50 = 1.0 nM 9.00
CHEMBL270057 IC50 = 1.0 nM 9.00
CHEMBL429430 IC50 = 1.0 nM 9.00
CHEMBL272875 IC50 = 1.0 nM 9.00
CHEMBL270306 IC50 = 1.0 nM 9.00
CHEMBL272822 IC50 = 3.0 nM 8.52
CHEMBL270550 IC50 = 19.0 nM 7.72
CHEMBL272170 IC50 = 26.0 nM 7.58
CHEMBL270093 IC50 = 26.0 nM 7.58
CHEMBL272609 IC50 = 40.0 nM 7.40
CHEMBL270545 IC50 = 40.0 nM 7.40
CHEMBL409933 IC50 = 40.0 nM 7.40
CHEMBL272874 IC50 = 53.0 nM 7.28
CHEMBL405040 IC50 = 58.0 nM 7.24
CHEMBL272688 IC50 = 62.0 nM 7.21
CHEMBL270953 IC50 = 77.0 nM 7.11
CHEMBL271960 IC50 = 95.0 nM 7.02