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Assay Detail

CHEMBL829417

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

Binding
Inhibition of Vascular endothelial growth factor receptor 2 (KDR)
45
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Isoindolinone ureas: a novel class of KDR kinase inhibitors.
Curtin ML, Frey RR, Heyman HR, Sarris KA, Steinman DH, Holmes JH, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Pease LJ, Glaser KB, Stewart KD, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2004) 14 : 4505 -4509
PubMed 15357981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.73 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410711 1 8.15
CHEMBL184274 1 8.00
CHEMBL183803 1 7.85
CHEMBL184971 1 7.75
CHEMBL183844 1 7.72
CHEMBL184223 1 7.68
CHEMBL184170 1 7.64
CHEMBL427321 1 7.54
CHEMBL185522 1 7.52
CHEMBL183174 1 7.47
CHEMBL427139 1 7.41
CHEMBL184706 1 7.36
CHEMBL182468 1 7.34
CHEMBL184847 1 7.30
CHEMBL185197 1 7.28
CHEMBL184021 1 7.19
CHEMBL185614 1 7.15
CHEMBL184226 1 7.08
CHEMBL185569 2 7.01
CHEMBL162 1 6.94
CHEMBL365448 1 6.90
CHEMBL364626 1 6.79
CHEMBL45651 1 6.58
CHEMBL359947 1 6.46
CHEMBL184143 1 6.43
CHEMBL181654 1 6.37
CHEMBL183025 1 6.33
CHEMBL182648 1 6.28
CHEMBL360032 1 6.24
CHEMBL185331 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410711 IC50 = 7.0 nM 8.15
CHEMBL184274 IC50 = 10.0 nM 8.00
CHEMBL183803 IC50 = 14.0 nM 7.85
CHEMBL184971 IC50 = 18.0 nM 7.75
CHEMBL183844 IC50 = 19.0 nM 7.72
CHEMBL184223 IC50 = 21.0 nM 7.68
CHEMBL184170 IC50 = 23.0 nM 7.64
CHEMBL427321 IC50 = 29.0 nM 7.54
CHEMBL185522 IC50 = 30.0 nM 7.52
CHEMBL183174 IC50 = 34.0 nM 7.47
CHEMBL427139 IC50 = 39.0 nM 7.41
CHEMBL184706 IC50 = 44.0 nM 7.36
CHEMBL182468 IC50 = 46.0 nM 7.34
CHEMBL184847 IC50 = 50.0 nM 7.30
CHEMBL185197 IC50 = 52.0 nM 7.28
CHEMBL184021 IC50 = 64.0 nM 7.19
CHEMBL185614 IC50 = 71.0 nM 7.15
CHEMBL184226 IC50 = 83.0 nM 7.08
CHEMBL185569 IC50 = 98.0 nM 7.01
CHEMBL185569 IC50 = 100.0 nM 7.00
CHEMBL162 IC50 = 115.0 nM 6.94
CHEMBL365448 IC50 = 126.0 nM 6.90
CHEMBL364626 IC50 = 161.0 nM 6.79
CHEMBL45651 IC50 = 263.0 nM 6.58
CHEMBL359947 IC50 = 350.0 nM 6.46
CHEMBL184143 IC50 = 370.0 nM 6.43
CHEMBL181654 IC50 = 430.0 nM 6.37
CHEMBL183025 IC50 = 470.0 nM 6.33
CHEMBL182648 IC50 = 520.0 nM 6.28
CHEMBL360032 IC50 = 570.0 nM 6.24
CHEMBL185331 IC50 = 770.0 nM 6.11
CHEMBL184997 IC50 = 1100.0 nM 5.96
CHEMBL185477 IC50 = 1800.0 nM 5.75
CHEMBL185477 IC50 = 1800.0 nM 5.75
CHEMBL359795 IC50 = 2100.0 nM 5.68
CHEMBL360724 IC50 = 4400.0 nM 5.36
CHEMBL184604 IC50 = 6000.0 nM 5.22
CHEMBL185059 IC50 = 9000.0 nM 5.05
CHEMBL183051 IC50 = 10000.0 nM 5.00
CHEMBL184918 IC50 = 19000.0 nM 4.72
CHEMBL183580 IC50 > 50000.0 nM -
CHEMBL185207 IC50 > 50000.0 nM -
CHEMBL185387 IC50 > 50000.0 nM -
CHEMBL361285 IC50 > 50000.0 nM -
CHEMBL297363 IC50 > 50.0 nM -