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Assay Detail

CHEMBL948355

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

Binding
Inhibition of human KDR phosphorylation expressed in mouse NIH3T3 cells by ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.
Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.
J Med Chem (2008) 51 : 3777 -3787
PubMed 18557606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.60 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453057 1 9.15
CHEMBL508928 1 9.00
CHEMBL453578 1 8.15
CHEMBL453058 1 8.10
CHEMBL469467 1 7.77
CHEMBL510814 1 7.68
CHEMBL452522 1 7.66
CHEMBL512839 1 7.55
CHEMBL469456 1 7.54
CHEMBL452783 1 7.48
CHEMBL510788 1 7.46
CHEMBL452288 1 7.31
CHEMBL469455 1 7.26
CHEMBL472302 1 7.16
CHEMBL452284 1 7.16
CHEMBL452287 1 7.07
CHEMBL507533 1 6.66
CHEMBL469468 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453057 IC50 = 0.7 nM 9.15
CHEMBL508928 IC50 = 1.0 nM 9.00
CHEMBL453578 IC50 = 7.0 nM 8.15
CHEMBL453058 IC50 = 8.0 nM 8.10
CHEMBL469467 IC50 = 17.0 nM 7.77
CHEMBL510814 IC50 = 21.0 nM 7.68
CHEMBL452522 IC50 = 22.0 nM 7.66
CHEMBL512839 IC50 = 28.0 nM 7.55
CHEMBL469456 IC50 = 29.0 nM 7.54
CHEMBL452783 IC50 = 33.0 nM 7.48
CHEMBL510788 IC50 = 35.0 nM 7.46
CHEMBL452288 IC50 = 49.0 nM 7.31
CHEMBL469455 IC50 = 55.0 nM 7.26
CHEMBL472302 IC50 = 70.0 nM 7.16
CHEMBL452284 IC50 = 70.0 nM 7.16
CHEMBL452287 IC50 = 86.0 nM 7.07
CHEMBL507533 IC50 = 220.0 nM 6.66
CHEMBL469468 IC50 = 250.0 nM 6.60