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Assay Detail

CHEMBL951280

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

Binding
Inhibition of KDR
24
Total Activities
24
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

Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R.
J Med Chem (2008) 51 : 1668 -1680
PubMed 18324759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.37 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272250 1 9.43
CHEMBL270342 1 9.35
CHEMBL429743 1 9.32
CHEMBL272198 1 9.22
CHEMBL271984 1 9.05
CHEMBL272252 1 8.92
CHEMBL260532 1 8.89
CHEMBL259252 1 8.89
CHEMBL269871 1 8.89
CHEMBL409103 1 8.89
CHEMBL270556 1 8.89
CHEMBL411284 1 8.54
CHEMBL410840 1 8.42
CHEMBL270754 1 8.42
CHEMBL271189 1 8.38
CHEMBL408211 1 8.23
CHEMBL270755 1 7.96
CHEMBL271188 1 7.92
CHEMBL428961 1 7.82
CHEMBL410903 1 7.82
CHEMBL260531 1 7.66
CHEMBL272251 1 7.55
CHEMBL412278 1 6.50
CHEMBL406914 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272250 IC50 = 0.37 nM 9.43
CHEMBL270342 IC50 = 0.45 nM 9.35
CHEMBL429743 IC50 = 0.48 nM 9.32
CHEMBL272198 IC50 = 0.6 nM 9.22
CHEMBL271984 IC50 = 0.9 nM 9.05
CHEMBL272252 IC50 = 1.2 nM 8.92
CHEMBL260532 IC50 = 1.3 nM 8.89
CHEMBL259252 IC50 = 1.3 nM 8.89
CHEMBL269871 IC50 = 1.3 nM 8.89
CHEMBL409103 IC50 = 1.3 nM 8.89
CHEMBL270556 IC50 = 1.3 nM 8.89
CHEMBL411284 IC50 = 2.9 nM 8.54
CHEMBL410840 IC50 = 3.8 nM 8.42
CHEMBL270754 IC50 = 3.8 nM 8.42
CHEMBL271189 IC50 = 4.2 nM 8.38
CHEMBL408211 IC50 = 5.9 nM 8.23
CHEMBL270755 IC50 = 11.0 nM 7.96
CHEMBL271188 IC50 = 12.0 nM 7.92
CHEMBL428961 IC50 = 15.0 nM 7.82
CHEMBL410903 IC50 = 15.0 nM 7.82
CHEMBL260531 IC50 = 22.0 nM 7.66
CHEMBL272251 IC50 = 28.0 nM 7.55
CHEMBL412278 IC50 = 314.0 nM 6.50
CHEMBL406914 IC50 = 1500.0 nM 5.82