Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5047434

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

Binding
Inhibition of JAK1/JAK3 signalling in human PBMC assessed as inhibition of IL-2 stimulated IFN-gamma release incubated for 1 hr followed by IL-2 stimulation by MSD assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PBMC
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK3/JAK1 (CHEMBL3038491)
Type PROTEIN COMPLEX
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 20 6.89 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5077126 1 7.60
CHEMBL5084542 1 7.60
CHEMBL5086526 1 7.50
CHEMBL5076189 1 7.40
CHEMBL5076068 1 7.30
CHEMBL5075556 1 7.20
CHEMBL5078647 1 7.10
CHEMBL5078141 1 7.10
CHEMBL5076101 1 6.90
CHEMBL5075673 1 6.90
CHEMBL5075223 1 6.90
CHEMBL5079248 1 6.80
CHEMBL5085176 1 6.60
CHEMBL5087255 1 6.60
CHEMBL5094089 1 6.60
CHEMBL5082928 1 6.50
CHEMBL5084340 1 6.40
CHEMBL5074310 1 6.30
CHEMBL5084913 1 6.30
CHEMBL5077653 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5077126 IC50 = 25.12 nM 7.60
CHEMBL5084542 IC50 = 25.12 nM 7.60
CHEMBL5086526 IC50 = 31.62 nM 7.50
CHEMBL5076189 IC50 = 39.81 nM 7.40
CHEMBL5076068 IC50 = 50.12 nM 7.30
CHEMBL5075556 IC50 = 63.1 nM 7.20
CHEMBL5078647 IC50 = 79.43 nM 7.10
CHEMBL5078141 IC50 = 79.43 nM 7.10
CHEMBL5076101 IC50 = 125.89 nM 6.90
CHEMBL5075673 IC50 = 125.89 nM 6.90
CHEMBL5075223 IC50 = 125.89 nM 6.90
CHEMBL5079248 IC50 = 158.49 nM 6.80
CHEMBL5085176 IC50 = 251.19 nM 6.60
CHEMBL5087255 IC50 = 251.19 nM 6.60
CHEMBL5094089 IC50 = 251.19 nM 6.60
CHEMBL5082928 IC50 = 316.23 nM 6.50
CHEMBL5084340 IC50 = 398.11 nM 6.40
CHEMBL5074310 IC50 = 501.19 nM 6.30
CHEMBL5084913 IC50 = 501.19 nM 6.30
CHEMBL5077653 IC50 = 630.96 nM 6.20