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Assay Detail

CHEMBL2066304

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

Binding
Inhibition of VEGFR1
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Hsu JT, Yeh TK, Yen SC, Chen CT, Hsieh SY, Hsu T, Lu CT, Chen CH, Chou LH, Chiu CH, Chang YI, Tseng YJ, Yen KR, Chao YS, Lin WH, Jiaang WT.
Bioorg Med Chem Lett (2012) 22 : 4654 -4659
PubMed 22726931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.77 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2063323 1 7.70
CHEMBL2063321 1 7.27
CHEMBL223360 LINIFANIB 3.0 1 7.16
CHEMBL2063324 1 7.16
CHEMBL2063436 1 7.09
CHEMBL1336 SORAFENIB 4.0 1 6.78
CHEMBL2063327 1 6.75
CHEMBL2063319 1 6.70
CHEMBL2063328 1 6.60
CHEMBL2063338 1 6.54
CHEMBL2063318 1 6.50
CHEMBL2063325 1 6.50
CHEMBL2063331 1 6.46
CHEMBL2063326 1 6.43
CHEMBL2063335 1 6.38
CHEMBL2063332 1 6.23
CHEMBL2063336 1 -
CHEMBL2063320 1 -
CHEMBL1807466 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL2063322 1 -
CHEMBL2063435 1 -
CHEMBL2063434 1 -
CHEMBL2063337 1 -
CHEMBL2063334 1 -
CHEMBL2063333 1 -
CHEMBL2063330 1 -
CHEMBL2063329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2063323 IC50 = 20.0 nM 7.70
CHEMBL2063321 IC50 = 54.0 nM 7.27
CHEMBL223360 LINIFANIB IC50 = 70.0 nM 7.16
CHEMBL2063324 IC50 = 70.0 nM 7.16
CHEMBL2063436 IC50 = 82.0 nM 7.09
CHEMBL1336 SORAFENIB IC50 = 165.0 nM 6.78
CHEMBL2063327 IC50 = 180.0 nM 6.75
CHEMBL2063319 IC50 = 200.0 nM 6.70
CHEMBL2063328 IC50 = 250.0 nM 6.60
CHEMBL2063338 IC50 = 290.0 nM 6.54
CHEMBL2063318 IC50 = 320.0 nM 6.50
CHEMBL2063325 IC50 = 320.0 nM 6.50
CHEMBL2063331 IC50 = 350.0 nM 6.46
CHEMBL2063326 IC50 = 370.0 nM 6.43
CHEMBL2063335 IC50 = 420.0 nM 6.38
CHEMBL2063332 IC50 = 590.0 nM 6.23
CHEMBL2063336 IC50 > 1000.0 nM -
CHEMBL2063320 IC50 > 1000.0 nM -
CHEMBL1807466 IC50 > 1000.0 nM -
CHEMBL576982 QUIZARTINIB IC50 > 10000.0 nM -
CHEMBL2063322 IC50 > 1000.0 nM -
CHEMBL2063435 IC50 > 1000.0 nM -
CHEMBL2063434 IC50 > 1000.0 nM -
CHEMBL2063337 IC50 > 1000.0 nM -
CHEMBL2063334 IC50 > 1000.0 nM -
CHEMBL2063333 IC50 > 1000.0 nM -
CHEMBL2063330 IC50 > 1000.0 nM -
CHEMBL2063329 IC50 > 1000.0 nM -