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Assay Detail

CHEMBL1073383

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

Binding
Inhibition of VEGFR3 by microplate scintillation counting
21
Total Activities
21
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 3 (CHEMBL1955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.
Tasler S, Müller O, Wieber T, Herz T, Pegoraro S, Saeb W, Lang M, Krauss R, Totzke F, Zirrgiebel U, Ehlert JE, Kubbutat MH, Schächtele C.
Bioorg Med Chem (2009) 17 : 6728 -6737
PubMed 19692247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.12 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595615 1 7.16
CHEMBL595143 1 6.92
CHEMBL595373 1 6.85
CHEMBL604483 1 6.72
CHEMBL593987 1 6.68
CHEMBL595406 1 6.47
CHEMBL594228 1 6.46
CHEMBL593274 1 6.33
CHEMBL606466 1 6.28
CHEMBL604992 1 6.06
CHEMBL596292 1 5.89
CHEMBL596087 1 5.82
CHEMBL593221 1 5.77
CHEMBL593306 1 5.72
CHEMBL593909 1 5.52
CHEMBL595142 1 5.35
CHEMBL593860 1 5.15
CHEMBL593275 1 5.03
CHEMBL593908 1 -
CHEMBL593770 1 -
CHEMBL593245 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595615 IC50 = 69.0 nM 7.16
CHEMBL595143 IC50 = 121.0 nM 6.92
CHEMBL595373 IC50 = 140.0 nM 6.85
CHEMBL604483 IC50 = 190.0 nM 6.72
CHEMBL593987 IC50 = 210.0 nM 6.68
CHEMBL595406 IC50 = 340.0 nM 6.47
CHEMBL594228 IC50 = 350.0 nM 6.46
CHEMBL593274 IC50 = 470.0 nM 6.33
CHEMBL606466 IC50 = 520.0 nM 6.28
CHEMBL604992 IC50 = 865.0 nM 6.06
CHEMBL596292 IC50 = 1300.0 nM 5.89
CHEMBL596087 IC50 = 1500.0 nM 5.82
CHEMBL593221 IC50 = 1700.0 nM 5.77
CHEMBL593306 IC50 = 1900.0 nM 5.72
CHEMBL593909 IC50 = 3000.0 nM 5.52
CHEMBL595142 IC50 = 4500.0 nM 5.35
CHEMBL593860 IC50 = 7100.0 nM 5.15
CHEMBL593275 IC50 = 9300.0 nM 5.03
CHEMBL593908 IC50 > 10000.0 nM -
CHEMBL593770 IC50 > 10000.0 nM -
CHEMBL593245 IC50 > 10000.0 nM -