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Assay Detail

CHEMBL1243976

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

Binding
Inhibition of recombinant VEGFR2 by radioactive phosphotransfer assay in presence of 10 uM ATP
209
Total Activities
209
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 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.
Nat Chem Biol (2008) 4 : 691 -699
PubMed 18849971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 209 5.65 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241676 1 8.37
CHEMBL1242295 1 8.05
CHEMBL1242026 1 8.00
CHEMBL1242662 1 8.00
CHEMBL1081312 1 7.92
CHEMBL1242293 1 7.72
CHEMBL1241484 1 7.70
CHEMBL1336 SORAFENIB 4.0 1 7.57
CHEMBL1242287 1 7.40
CHEMBL1242109 1 7.37
CHEMBL1242285 1 7.36
CHEMBL1242199 1 7.32
CHEMBL1242376 1 7.26
CHEMBL1241578 1 7.26
CHEMBL1242202 1 7.26
CHEMBL1241580 1 7.21
CHEMBL1241678 1 7.18
CHEMBL1242377 1 7.17
CHEMBL1242294 1 7.12
CHEMBL1242656 1 7.11
CHEMBL1242198 1 7.03
CHEMBL535 SUNITINIB 4.0 1 7.02
CHEMBL1241768 1 6.99
CHEMBL1242568 1 6.97
CHEMBL1242289 1 6.96
CHEMBL1242114 1 6.92
CHEMBL1242664 1 6.87
CHEMBL1241271 1 6.82
CHEMBL1242852 1 6.82
CHEMBL1241677 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241676 IC50 = 4.3 nM 8.37
CHEMBL1242295 IC50 = 9.0 nM 8.05
CHEMBL1242026 IC50 = 10.0 nM 8.00
CHEMBL1242662 IC50 = 10.0 nM 8.00
CHEMBL1081312 IC50 = 12.0 nM 7.92
CHEMBL1242293 IC50 = 19.0 nM 7.72
CHEMBL1241484 IC50 = 20.0 nM 7.70
CHEMBL1336 SORAFENIB IC50 = 27.0 nM 7.57
CHEMBL1242287 IC50 = 40.0 nM 7.40
CHEMBL1242109 IC50 = 43.0 nM 7.37
CHEMBL1242285 IC50 = 44.0 nM 7.36
CHEMBL1242199 IC50 = 48.0 nM 7.32
CHEMBL1241578 IC50 = 55.0 nM 7.26
CHEMBL1242376 IC50 = 55.0 nM 7.26
CHEMBL1242202 IC50 = 55.0 nM 7.26
CHEMBL1241580 IC50 = 62.0 nM 7.21
CHEMBL1241678 IC50 = 66.0 nM 7.18
CHEMBL1242377 IC50 = 68.0 nM 7.17
CHEMBL1242294 IC50 = 76.0 nM 7.12
CHEMBL1242656 IC50 = 77.0 nM 7.11
CHEMBL1242198 IC50 = 93.0 nM 7.03
CHEMBL535 SUNITINIB IC50 = 95.0 nM 7.02
CHEMBL1241768 IC50 = 103.0 nM 6.99
CHEMBL1242568 IC50 = 106.0 nM 6.97
CHEMBL1242289 IC50 = 109.0 nM 6.96
CHEMBL1242114 IC50 = 119.0 nM 6.92
CHEMBL1242664 IC50 = 134.0 nM 6.87
CHEMBL1242852 IC50 = 153.0 nM 6.82
CHEMBL1241271 IC50 = 151.0 nM 6.82
CHEMBL1241677 IC50 = 174.0 nM 6.76
CHEMBL1242385 IC50 = 172.0 nM 6.76
CHEMBL1242750 IC50 = 178.0 nM 6.75
CHEMBL1241486 IC50 = 194.0 nM 6.71
CHEMBL1242573 IC50 = 215.0 nM 6.67
CHEMBL1242024 IC50 = 213.0 nM 6.67
CHEMBL1230790 IC50 = 213.0 nM 6.67
CHEMBL1241270 IC50 = 237.0 nM 6.62
CHEMBL1242201 IC50 = 259.0 nM 6.59
CHEMBL1242113 IC50 = 279.0 nM 6.55
CHEMBL1242386 IC50 = 295.0 nM 6.53
CHEMBL1233882 IC50 = 310.0 nM 6.51
CHEMBL1242572 IC50 = 330.0 nM 6.48
CHEMBL1242657 IC50 = 369.0 nM 6.43
CHEMBL1242748 IC50 = 401.0 nM 6.40
CHEMBL1242475 IC50 = 411.0 nM 6.39
CHEMBL1242477 IC50 = 420.0 nM 6.38
CHEMBL1241770 IC50 = 435.0 nM 6.36
CHEMBL1242574 IC50 = 470.0 nM 6.33
CHEMBL1242566 IC50 = 517.0 nM 6.29
CHEMBL1242661 IC50 = 550.0 nM 6.26