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Assay Detail

CHEMBL907547

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Functional
Inhibition of human KDR phosphorylation in NIH3T3 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Thienopyridine urea inhibitors of KDR kinase.
Heyman HR, Frey RR, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Yates M, Bouska JJ, Albert DH, Black-Schaefer CL, Dandliker PJ, Stewart KD, Rafferty P, Davidsen SK, Michaelides MR, Curtin ML.
Bioorg Med Chem Lett (2007) 17 : 1246 -1249
PubMed 17188869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.42 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231127 1 9.00
CHEMBL268826 1 8.40
CHEMBL427267 1 8.40
CHEMBL231411 1 7.82
CHEMBL398196 1 7.54
CHEMBL231109 1 7.50
CHEMBL394619 1 7.50
CHEMBL231511 1 7.48
CHEMBL231308 1 7.39
CHEMBL396737 1 7.32
CHEMBL231309 1 7.32
CHEMBL231612 1 7.25
CHEMBL394790 1 7.25
CHEMBL231412 1 7.21
CHEMBL231255 1 7.14
CHEMBL231456 1 6.85
CHEMBL231209 1 6.83
CHEMBL396494 1 6.70
CHEMBL231410 1 6.05
CHEMBL231415 1 -
CHEMBL394789 1 -
CHEMBL231310 1 -
CHEMBL231128 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231127 IC50 = 1.0 nM 9.00
CHEMBL268826 IC50 = 4.0 nM 8.40
CHEMBL427267 IC50 = 4.0 nM 8.40
CHEMBL231411 IC50 = 15.0 nM 7.82
CHEMBL398196 IC50 = 29.0 nM 7.54
CHEMBL231109 IC50 = 32.0 nM 7.50
CHEMBL394619 IC50 = 32.0 nM 7.50
CHEMBL231511 IC50 = 33.0 nM 7.48
CHEMBL231308 IC50 = 41.0 nM 7.39
CHEMBL396737 IC50 = 48.0 nM 7.32
CHEMBL231309 IC50 = 48.0 nM 7.32
CHEMBL231612 IC50 = 56.0 nM 7.25
CHEMBL394790 IC50 = 56.0 nM 7.25
CHEMBL231412 IC50 = 61.0 nM 7.21
CHEMBL231255 IC50 = 72.0 nM 7.14
CHEMBL231456 IC50 = 141.0 nM 6.85
CHEMBL231209 IC50 = 147.0 nM 6.83
CHEMBL396494 IC50 = 198.0 nM 6.70
CHEMBL231410 IC50 = 895.0 nM 6.05
CHEMBL231415 IC50 - -
CHEMBL394789 IC50 - -
CHEMBL231310 IC50 - -
CHEMBL231128 IC50 - -