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Assay Detail

CHEMBL932834

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

Binding
Inhibition of KDR by HTRF assay
ChEMBL ↗
46
Total Activities
46
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

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R.
J Med Chem (2008) 51 : 1649 -1667
PubMed 18324761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 8.69 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272824 — — 1 9.70
CHEMBL409538 — — 1 9.70
CHEMBL409512 — — 1 9.70
CHEMBL429585 — — 1 9.52
CHEMBL270092 — — 1 9.52
CHEMBL269916 — — 1 9.52
CHEMBL272691 — — 1 9.52
CHEMBL429743 — — 1 9.30
CHEMBL270985 — — 1 9.30
CHEMBL271563 — — 1 9.30
CHEMBL411091 — — 1 9.30
CHEMBL272198 — — 1 9.22
CHEMBL259461 — — 1 9.22
CHEMBL412291 — — 1 9.22
CHEMBL407715 — — 1 9.15
CHEMBL408478 — — 1 9.10
CHEMBL269915 — — 1 9.10
CHEMBL406388 — — 1 9.10
CHEMBL270978 — — 1 9.00
CHEMBL273062 — — 1 9.00
CHEMBL269914 — — 1 9.00
CHEMBL410841 — — 1 9.00
CHEMBL409103 — — 1 8.89
CHEMBL270547 — — 1 8.70
CHEMBL270983 — — 1 8.70
CHEMBL272823 — — 1 8.70
CHEMBL272693 — — 1 8.70
CHEMBL221484 — — 1 8.70
CHEMBL271181 — — 1 8.52
CHEMBL259252 — — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272824 — IC50 = 0.2 nM 9.70
CHEMBL409538 — IC50 = 0.2 nM 9.70
CHEMBL409512 — IC50 = 0.2 nM 9.70
CHEMBL429585 — IC50 = 0.3 nM 9.52
CHEMBL270092 — IC50 = 0.3 nM 9.52
CHEMBL269916 — IC50 = 0.3 nM 9.52
CHEMBL272691 — IC50 = 0.3 nM 9.52
CHEMBL411091 — IC50 = 0.5 nM 9.30
CHEMBL429743 — IC50 = 0.5 nM 9.30
CHEMBL271563 — IC50 = 0.5 nM 9.30
CHEMBL270985 — IC50 = 0.5 nM 9.30
CHEMBL412291 — IC50 = 0.6 nM 9.22
CHEMBL259461 — IC50 = 0.6 nM 9.22
CHEMBL272198 — IC50 = 0.6 nM 9.22
CHEMBL407715 — IC50 = 0.7 nM 9.15
CHEMBL408478 — IC50 = 0.8 nM 9.10
CHEMBL406388 — IC50 = 0.8 nM 9.10
CHEMBL269915 — IC50 = 0.8 nM 9.10
CHEMBL270978 — IC50 = 1.0 nM 9.00
CHEMBL273062 — IC50 = 1.0 nM 9.00
CHEMBL269914 — IC50 = 1.0 nM 9.00
CHEMBL410841 — IC50 = 1.0 nM 9.00
CHEMBL409103 — IC50 = 1.3 nM 8.89
CHEMBL270547 — IC50 = 2.0 nM 8.70
CHEMBL221484 — IC50 = 2.0 nM 8.70
CHEMBL272693 — IC50 = 2.0 nM 8.70
CHEMBL270983 — IC50 = 2.0 nM 8.70
CHEMBL272823 — IC50 = 2.0 nM 8.70
CHEMBL271181 — IC50 = 3.0 nM 8.52
CHEMBL259252 — IC50 = 3.0 nM 8.52
CHEMBL429410 — IC50 = 3.0 nM 8.52
CHEMBL273064 — IC50 = 4.0 nM 8.40
CHEMBL408211 — IC50 = 5.0 nM 8.30
CHEMBL272827 — IC50 = 7.0 nM 8.15
CHEMBL270277 — IC50 = 8.0 nM 8.10
CHEMBL410903 — IC50 = 9.0 nM 8.05
CHEMBL428961 — IC50 = 15.0 nM 7.82
CHEMBL269891 — IC50 = 18.0 nM 7.75
CHEMBL272449 — IC50 = 20.0 nM 7.70
CHEMBL272670 — IC50 = 20.0 nM 7.70
CHEMBL270745 — IC50 = 22.0 nM 7.66
CHEMBL446367 — IC50 = 23.0 nM 7.64
CHEMBL410093 — IC50 = 28.0 nM 7.55
CHEMBL413933 — IC50 = 46.0 nM 7.34
CHEMBL270258 — IC50 = 310.0 nM 6.51
CHEMBL271414 — IC50 > 1400.0 nM -