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Assay Detail

CHEMBL2162415

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

Binding
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 45 mins in presence of human whole blood
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Cell Type TF-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.
J Med Chem (2012) 55 : 6176 -6193
PubMed 22698084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.80 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159210 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159210 EC50 = 160.0 nM 6.80