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Assay Detail

CHEMBL5047431

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

Binding
Inhibition of human GST/6His-tagged VEGFR2 using Biotin-aminohexyl-EEEEYFELVAKKKK-NH2 as substrate incubated for 90 mins in presence of ATP by TR-FRET assay
22
Total Activities
22
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 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Wellaway CR, Baldwin IR, Bamborough P, Barker D, Bartholomew MA, Chung CW, Dümpelfeld B, Evans JP, Fazakerley NJ, Homes P, Keeling SP, Lewell XQ, McNab FW, Morley J, Needham D, Neu M, van Oosterhout AJM, Pal A, Reinhard FBM, Rianjongdee F, Robertson CM, Rowland P, Shah RR, Sherriff EB, Sloan LA, Teague S, Thomas DA, Wellaway N, Wojno-Picon J, Woolven JM, Coe DM.
J Med Chem (2022) 65 : 633 -664
PubMed 34928601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.18 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079248 1 7.10
CHEMBL5075556 1 7.00
CHEMBL5076189 1 6.90
CHEMBL5086526 1 6.70
CHEMBL5088804 1 6.40
CHEMBL5087255 1 6.30
CHEMBL5084542 1 6.20
CHEMBL5078647 1 6.20
CHEMBL5078141 1 6.20
CHEMBL5077126 1 6.20
CHEMBL5075223 1 6.20
CHEMBL5076101 1 6.10
CHEMBL5094089 1 6.00
CHEMBL5075673 1 6.00
CHEMBL5084340 1 6.00
CHEMBL5085176 1 5.90
CHEMBL5074310 1 5.90
CHEMBL5084913 1 5.90
CHEMBL5082928 1 5.80
CHEMBL5077653 1 5.70
CHEMBL5076068 1 5.60
CHEMBL5089877 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079248 IC50 = 79.43 nM 7.10
CHEMBL5075556 IC50 = 100.0 nM 7.00
CHEMBL5076189 IC50 = 125.89 nM 6.90
CHEMBL5086526 IC50 = 199.53 nM 6.70
CHEMBL5088804 IC50 = 398.11 nM 6.40
CHEMBL5087255 IC50 = 501.19 nM 6.30
CHEMBL5084542 IC50 = 630.96 nM 6.20
CHEMBL5078647 IC50 = 630.96 nM 6.20
CHEMBL5078141 IC50 = 630.96 nM 6.20
CHEMBL5077126 IC50 = 630.96 nM 6.20
CHEMBL5075223 IC50 = 630.96 nM 6.20
CHEMBL5076101 IC50 = 794.33 nM 6.10
CHEMBL5094089 IC50 = 1000.0 nM 6.00
CHEMBL5075673 IC50 = 1000.0 nM 6.00
CHEMBL5084340 IC50 = 1000.0 nM 6.00
CHEMBL5085176 IC50 = 1258.93 nM 5.90
CHEMBL5074310 IC50 = 1258.93 nM 5.90
CHEMBL5084913 IC50 = 1258.93 nM 5.90
CHEMBL5082928 IC50 = 1584.89 nM 5.80
CHEMBL5077653 IC50 = 1995.26 nM 5.70
CHEMBL5076068 IC50 = 2511.89 nM 5.60
CHEMBL5089877 IC50 = 2511.89 nM 5.60