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Assay Detail

CHEMBL864249

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Functional
Inhibition of KDR by cellular assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2006) 16 : 4326 -4330
PubMed 16735117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.64 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196363 1 9.00
CHEMBL376951 1 9.00
CHEMBL213504 1 8.30
CHEMBL445570 1 8.30
CHEMBL262433 1 7.68
CHEMBL379372 1 7.30
CHEMBL211378 1 7.00
CHEMBL213505 1 6.77
CHEMBL210003 1 6.60
CHEMBL378687 1 6.42
CHEMBL214258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196363 IC50 = 1.0 nM 9.00
CHEMBL376951 IC50 = 1.0 nM 9.00
CHEMBL213504 IC50 = 5.0 nM 8.30
CHEMBL445570 IC50 = 5.0 nM 8.30
CHEMBL262433 IC50 = 21.0 nM 7.68
CHEMBL379372 IC50 = 50.0 nM 7.30
CHEMBL211378 IC50 = 100.0 nM 7.00
CHEMBL213505 IC50 = 170.0 nM 6.77
CHEMBL210003 IC50 = 250.0 nM 6.60
CHEMBL378687 IC50 = 385.0 nM 6.42
CHEMBL214258 IC50 - -