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Assay Detail

CHEMBL5507224

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

Binding
Inhibition of JAK1 in mouse Ba/F3-TEL-JAK1 cells assessed as inhibition of JAK1-driven cell growth incubated for 72 hrs by CCK8 assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Ba/F3-TEL-JAK1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK1 (CHEMBL2968)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.
Chen L, Tang Y, Lang JJ, Lin Y, Yu Z, Li X, Zheng X, Mi P, Lv Y, Lin YW.
Eur J Med Chem (2024) 267 : 116210 -116210
PubMed 38359535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.64 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5542400 1 6.92
CHEMBL5563563 1 6.64
CHEMBL221959 TOFACITINIB 4.0 1 6.59
CHEMBL5566342 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5542400 IC50 = 120.0 nM 6.92
CHEMBL5563563 IC50 = 230.0 nM 6.64
CHEMBL221959 TOFACITINIB IC50 = 258.0 nM 6.59
CHEMBL5566342 IC50 = 408.0 nM 6.39