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Assay Detail

CHEMBL5047426

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

Binding
Inhibition of GST-fused human JAK1 (854 to 1154 residues) expressed in insect cells using ULight-JAK-1 Tyr1023 peptide as substrate preincubated for 30 mins followed by substrate addition and further incubated for 20 mins in presence of ATP by FRET assay
31
Total Activities
31
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

Tyrosine-protein kinase JAK1 (CHEMBL2835)
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 31 8.34 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5076189 1 9.50
CHEMBL5086526 1 9.40
CHEMBL5078647 1 9.30
CHEMBL5084861 1 9.30
CHEMBL5078141 1 9.30
CHEMBL5075556 1 9.20
CHEMBL5075673 1 9.20
CHEMBL5084542 1 9.10
CHEMBL5085176 1 9.00
CHEMBL5084340 1 8.90
CHEMBL5079248 1 8.90
CHEMBL5082928 1 8.90
CHEMBL5076068 1 8.80
CHEMBL5077126 1 8.80
CHEMBL5074310 1 8.70
CHEMBL5087255 1 8.70
CHEMBL5077653 1 8.60
CHEMBL5075223 1 8.60
CHEMBL5084913 1 8.40
CHEMBL5094089 1 8.30
CHEMBL5076101 1 8.30
CHEMBL5089877 1 8.10
CHEMBL5076598 1 8.10
CHEMBL5079734 1 7.90
CHEMBL5088804 1 7.50
CHEMBL5074436 1 7.20
CHEMBL5072425 1 7.10
CHEMBL5084809 1 6.90
CHEMBL5075565 1 6.60
CHEMBL5073925 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5076189 IC50 = 0.3162 nM 9.50
CHEMBL5086526 IC50 = 0.3981 nM 9.40
CHEMBL5078647 IC50 = 0.5012 nM 9.30
CHEMBL5084861 IC50 = 0.5012 nM 9.30
CHEMBL5078141 IC50 = 0.5012 nM 9.30
CHEMBL5075556 IC50 = 0.631 nM 9.20
CHEMBL5075673 IC50 = 0.631 nM 9.20
CHEMBL5084542 IC50 = 0.7943 nM 9.10
CHEMBL5085176 IC50 = 1.0 nM 9.00
CHEMBL5084340 IC50 = 1.259 nM 8.90
CHEMBL5079248 IC50 = 1.259 nM 8.90
CHEMBL5082928 IC50 = 1.259 nM 8.90
CHEMBL5076068 IC50 = 1.585 nM 8.80
CHEMBL5077126 IC50 = 1.585 nM 8.80
CHEMBL5074310 IC50 = 1.995 nM 8.70
CHEMBL5087255 IC50 = 1.995 nM 8.70
CHEMBL5077653 IC50 = 2.512 nM 8.60
CHEMBL5075223 IC50 = 2.512 nM 8.60
CHEMBL5084913 IC50 = 3.981 nM 8.40
CHEMBL5094089 IC50 = 5.012 nM 8.30
CHEMBL5076101 IC50 = 5.012 nM 8.30
CHEMBL5089877 IC50 = 7.943 nM 8.10
CHEMBL5076598 IC50 = 7.943 nM 8.10
CHEMBL5079734 IC50 = 12.59 nM 7.90
CHEMBL5088804 IC50 = 31.62 nM 7.50
CHEMBL5074436 IC50 = 63.1 nM 7.20
CHEMBL5072425 IC50 = 79.43 nM 7.10
CHEMBL5084809 IC50 = 125.89 nM 6.90
CHEMBL5075565 IC50 = 251.19 nM 6.60
CHEMBL5073925 IC50 = 630.96 nM 6.20
CHEMBL5076662 IC50 = 1584.89 nM 5.80