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Assay Detail

CHEMBL2390364

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

Binding
Inhibition of TYK2 in human NK92 cells assessed as inhibition of IL12-induced STAT4 phosphorylation incubated for 20 mins followed by IL12 challenge for 45 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NK92
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ.
J Med Chem (2013) 56 : 4764 -4785
PubMed 23659214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.10 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386635 1 7.00
CHEMBL2386629 1 6.51
CHEMBL221959 TOFACITINIB 4.0 1 6.15
CHEMBL2386636 1 6.01
CHEMBL2385096 1 5.66
CHEMBL2386633 1 5.25
CHEMBL2386653 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386635 EC50 = 100.0 nM 7.00
CHEMBL2386629 EC50 = 310.0 nM 6.51
CHEMBL221959 TOFACITINIB EC50 = 710.0 nM 6.15
CHEMBL2386636 EC50 = 980.0 nM 6.01
CHEMBL2385096 EC50 = 2200.0 nM 5.66
CHEMBL2386633 EC50 = 5600.0 nM 5.25
CHEMBL2386653 EC50 > 5800.0 nM -