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Assay Detail

CHEMBL861908

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

Binding
Inhibitory activity against VEGFR1 by HTRF assay
35
Total Activities
35
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 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.
Kiselyov AS, Piatnitski E, Semenova M, Semenov VV.
Bioorg Med Chem Lett (2006) 16 : 602 -606
PubMed 16275072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.93 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24828 VANDETANIB 4.0 1 7.00
CHEMBL101253 VATALANIB 3.0 1 6.85
CHEMBL202011 1 6.80
CHEMBL153843 1 6.77
CHEMBL205114 1 6.51
CHEMBL383215 1 6.23
CHEMBL202153 1 6.20
CHEMBL202466 1 6.14
CHEMBL202384 1 6.14
CHEMBL370600 1 6.12
CHEMBL379674 1 6.12
CHEMBL201906 1 6.08
CHEMBL202408 1 5.63
CHEMBL382308 1 5.52
CHEMBL201713 1 5.42
CHEMBL203095 1 5.34
CHEMBL380700 1 5.33
CHEMBL202714 1 5.27
CHEMBL202109 1 5.27
CHEMBL201014 1 5.26
CHEMBL201659 1 5.19
CHEMBL203149 1 5.16
CHEMBL202234 1 -
CHEMBL381300 1 -
CHEMBL205113 1 -
CHEMBL377921 1 -
CHEMBL202383 1 -
CHEMBL201712 1 -
CHEMBL424672 1 -
CHEMBL382184 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24828 VANDETANIB IC50 = 100.0 nM 7.00
CHEMBL101253 VATALANIB IC50 = 140.0 nM 6.85
CHEMBL202011 IC50 = 160.0 nM 6.80
CHEMBL153843 IC50 = 170.0 nM 6.77
CHEMBL205114 IC50 = 310.0 nM 6.51
CHEMBL383215 IC50 = 590.0 nM 6.23
CHEMBL202153 IC50 = 630.0 nM 6.20
CHEMBL202466 IC50 = 720.0 nM 6.14
CHEMBL202384 IC50 = 720.0 nM 6.14
CHEMBL370600 IC50 = 750.0 nM 6.12
CHEMBL379674 IC50 = 760.0 nM 6.12
CHEMBL201906 IC50 = 840.0 nM 6.08
CHEMBL202408 IC50 = 2330.0 nM 5.63
CHEMBL382308 IC50 = 3020.0 nM 5.52
CHEMBL201713 IC50 = 3850.0 nM 5.42
CHEMBL203095 IC50 = 4600.0 nM 5.34
CHEMBL380700 IC50 = 4660.0 nM 5.33
CHEMBL202714 IC50 = 5420.0 nM 5.27
CHEMBL202109 IC50 = 5320.0 nM 5.27
CHEMBL201014 IC50 = 5460.0 nM 5.26
CHEMBL201659 IC50 = 6410.0 nM 5.19
CHEMBL203149 IC50 = 6850.0 nM 5.16
CHEMBL383575 IC50 > 10000.0 nM -
CHEMBL201303 IC50 > 10000.0 nM -
CHEMBL425930 IC50 > 10000.0 nM -
CHEMBL382647 IC50 > 10000.0 nM -
CHEMBL203698 IC50 > 10000.0 nM -
CHEMBL382184 IC50 > 10000.0 nM -
CHEMBL424672 IC50 > 10000.0 nM -
CHEMBL201712 IC50 > 10000.0 nM -
CHEMBL202383 IC50 > 10000.0 nM -
CHEMBL377921 IC50 > 10000.0 nM -
CHEMBL205113 IC50 > 10000.0 nM -
CHEMBL381300 IC50 > 10000.0 nM -
CHEMBL202234 IC50 > 10000.0 nM -